Search Result
Results for "
Selective antagonist
" in MedChemExpress (MCE) Product Catalog:
2069
Inhibitors & Agonists
1
Biochemical Assay Reagents
85
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108530
-
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RAR/RXR
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Cancer
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MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
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-
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- HY-107327
-
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(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
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Cardiovascular Disease
|
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Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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-
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- HY-122136
-
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Melatonin Receptor
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Neurological Disease
|
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S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist .
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-
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- HY-126123
-
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iGluR
Potassium Channel
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Neurological Disease
|
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NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
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-
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- HY-153990
-
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FKBP
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Neurological Disease
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FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52 .
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-
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- HY-115413
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-
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- HY-107327R
-
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Adrenergic Receptor
|
Cardiovascular Disease
|
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Carazolol (Standard) is the analytical standard of Carazolol. This product is intended for research and analytical applications. Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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-
-
- HY-117634
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-
-
- HY-12819
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-
-
- HY-116386
-
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Histamine Receptor
|
Neurological Disease
|
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GSK334429 is a selective and orally active non-imidazole histamine H3 receptor antagonist with a pKi of 9.49 against human H3 receptor. GSK334429 can be utilized in neurological research .
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-
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- HY-14431A
-
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SAM-531 hydrochloride; PF-05212365 hydrochloride
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5-HT Receptor
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Neurological Disease
|
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Cerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease .
|
-
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- HY-12908
-
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Bcl-2 Family
Apoptosis
|
Cancer
|
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Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL) .
|
-
-
- HY-14431
-
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SAM-531; PF-05212365
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5-HT Receptor
|
Neurological Disease
|
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Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease .
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-
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- HY-116908
-
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5-HT Receptor
|
Neurological Disease
|
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SB-272183 is a selective 5-HT1A, 5-HT1B and 5-HT1D receptor antagonist. In addition, SB-272183 is also a potent and selective ligand for 5-HT1A, 5-HT1B and 5-HT1D receptors in human recombinant and native tissues with pKi values ??of 8.0, 8.1 and 8.7, respectively. SB-272183 can be used in antidepressant research .
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- HY-151413
-
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Neurokinin Receptor
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Neurological Disease
|
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MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
|
-
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- HY-P10571
-
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Melanocortin Receptor
|
Endocrinology
|
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GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
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- HY-19057
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MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
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Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
|
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- HY-118944
-
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Adrenergic Receptor
|
Endocrinology
|
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L-748328 is a potent and selective human β3-adrenergic receptor antagonist. L-748328 has a Ki of 3.7 nM against human cloned β3-AR expressed in Chinese hamster ovary (CHO) cells. In addition, L-748328 inhibits the lipolytic response induced by the β3-AR agonist L-742791 in isolated non-human primate adipocytes .
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- HY-106684
-
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Adrenergic Receptor
|
Cardiovascular Disease
|
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Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
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- HY-106684A
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Adrenergic Receptor
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Cardiovascular Disease
|
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Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
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- HY-137955
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P2Y Receptor
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Cardiovascular Disease
Others
Neurological Disease
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MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC50= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system .
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- HY-135783
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nAChR
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Neurological Disease
|
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AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
|
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- HY-145341
-
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Estrogen Receptor/ERR
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Cancer
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GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
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- HY-P10388
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CD47
TGF-β Receptor
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Cancer
|
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TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
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- HY-112562
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- HY-112264
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- HY-103650
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- HY-103651
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Oxytocin Receptor
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Endocrinology
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OT antagonist 1 demethyl derivative is the demethyl derivative of OT antagonist 1. OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
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- HY-111500
-
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iGluR
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Neurological Disease
|
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(Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist .
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- HY-139675
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-
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- HY-147392
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CXCR
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Metabolic Disease
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CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research .
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- HY-113973
-
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LPL Receptor
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Cancer
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LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM) .
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- HY-15015
-
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Oxytocin receptor antagonist 1
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Oxytocin Receptor
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Endocrinology
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OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
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- HY-145905
-
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Dopamine Receptor
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Neurological Disease
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D4R antagonist-1 is a potent and selective D4R antagonist with an IC50 of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease .
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- HY-147398
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Dopamine Receptor
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Neurological Disease
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Dopamine D4 receptor antagonist-1 is a selective DRD4 antagonists, with a Ki of 9.0 nM for Hd4.2. Dopamine D4 receptor antagonist-1 can be used in study of schizophrenia .
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- HY-101574
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- HY-106910
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- HY-120652
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Adenosine Receptor
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Inflammation/Immunology
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A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors .
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- HY-111500A
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- HY-129995A
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TSH Receptor
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Endocrinology
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TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy .
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- HY-141865
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aR than A2bR.
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- HY-18076
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- HY-153165
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Others
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Others
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RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.
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- HY-13209
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- HY-100903
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nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
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Opioid Receptor
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Neurological Disease
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Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
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- HY-112430
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TRP Channel
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Neurological Disease
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TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
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- HY-146517
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1) .
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- HY-163694
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Adrenergic Receptor
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Inflammation/Immunology
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ADRA2A antagonist 1 (compd 4n) is a potent and selective ADRA2A antagonist with an IC50 of 18 nM. ADRA2A antagonist 1 can be used for inflammation and sepsis research .
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- HY-141609
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Aryl Hydrocarbon Receptor
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Cancer
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AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases .
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- HY-101745
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- HY-U00234
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- HY-112620
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- HY-110110
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- HY-107602
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- HY-U00368
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- HY-110203
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TNF-α antagonist III
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TNF Receptor
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Cancer
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R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
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- HY-126217
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- HY-22437S
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- HY-162267
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LPL Receptor
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Inflammation/Immunology
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LPAR1 antagonist 1 (compound 18) is a potent, oral active and selective LPAR1 antagonist with the IC50 of 3.3 nM. LPAR1 antagonist 1 can be used for study of fibrosis .
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- HY-163701
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Adenosine Receptor
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Cancer
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hA2AAR antagonist 1 (compound 4a) is a highly selective hA2AAR antagonist with a Ki of 5 nM. hA2AAR antagonist 1 can be used in the study of immune-oncology .
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- HY-151481
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FXR
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Metabolic Disease
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FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
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- HY-145906
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Dopamine Receptor
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Neurological Disease
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D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .
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- HY-103456
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- HY-135270
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- HY-124759
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CCR
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Inflammation/Immunology
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CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC50 of 6.8 nM in calcium flux assay .
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- HY-22437S1
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- HY-112628
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AHR antagonist 7
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Aryl Hydrocarbon Receptor
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Cancer
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CAY10464 (AHR antagonist 7; compound 4j) is a selective and high-affinity aryl hydrocarbon receptor (AhR) antagonist with a Ki of 1.4 nM .
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- HY-131868
-
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TRP Channel
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Neurological Disease
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TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain .
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- HY-15085
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- HY-18101A
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- HY-16763
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- HY-14778
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- HY-101602
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- HY-19973
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- HY-116859
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- HY-14277A
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R 50547 hydrochloride
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Histamine Receptor
Neurotensin Receptor
Integrin
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Inflammation/Immunology
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Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
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- HY-14277
-
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R 50547
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Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
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Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
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- HY-107716
-
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iGluR
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Neurological Disease
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Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist .
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- HY-164621
-
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Adenosine Receptor
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Others
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A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM .
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- HY-107748A
-
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5'-GNTI TFA
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Others
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Neurological Disease
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5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .
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- HY-B1416A
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- HY-P3854
-
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Neurokinin Receptor
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Neurological Disease
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GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
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- HY-147226
-
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Prostaglandin Receptor
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Neurological Disease
Endocrinology
|
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EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research .
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- HY-161420
-
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TRP Channel
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Neurological Disease
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TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 antagonist that effectively blocks capsaicin activation (IC50=2.31 nM). TRPV1 antagonist 7 can be used in analgesic research .
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- HY-U00018
-
-
- HY-50663
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MK 0893
5 Publications Verification
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GCGR
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Metabolic Disease
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MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.
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- HY-A0066
-
-
- HY-19737A
-
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PPAR
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Cancer
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DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
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- HY-101502A
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-
- HY-13439
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-
- HY-42849A
-
-
- HY-42849
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-
- HY-15487
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-
- HY-12114
-
-
- HY-P1782
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- HY-22437
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(±)-UK-88525
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mAChR
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Neurological Disease
Cancer
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(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist .
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- HY-125145
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-
- HY-P1018
-
-
- HY-12701
-
-
- HY-15277
-
-
- HY-156280
-
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RAR/RXR
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Endocrinology
|
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RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM .
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- HY-163091
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- HY-152581
-
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Cannabinoid Receptor
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Inflammation/Immunology
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CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines .
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- HY-144372
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TRP Channel
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Neurological Disease
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TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
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- HY-157455
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Androgen Receptor
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Cancer
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AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
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- HY-168141
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC50=18 nM). .
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- HY-118918
-
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Vasopressin Receptor
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Endocrinology
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YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease .
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- HY-155185
-
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iGluR
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Neurological Disease
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NMDA receptor antagonist 7 (Compound (S)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 93 nM and an IC50 of 72 nM. NMDA receptor antagonist 7 can be used for research of neurodegenerative diseases .
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- HY-155185A
-
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iGluR
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Neurological Disease
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NMDA receptor antagonist 8 (Compound (R)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 265 nM and an IC50 of 62 nM. NMDA receptor antagonist 8 can be used for research of neurodegenerative diseases .
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- HY-114427
-
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iGluR
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Neurological Disease
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NS-102 is a selective kainate (GluK2) receptor antagonist. NS-102 is a potent GluR6/7 receptor antagonist .
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-
- HY-144672
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-
- HY-101306
-
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Opioid Receptor
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Neurological Disease
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Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors .
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-
- HY-157493
-
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Progesterone Receptor
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Endocrinology
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PR antagonist 1 (compound 8) is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids .
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- HY-159895
-
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
|
|
PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice .
|
-
- HY-19684
-
-
- HY-14390
-
-
- HY-50691
-
-
- HY-50912
-
-
- HY-76520
-
-
- HY-12510
-
-
- HY-15709
-
-
- HY-15574A
-
-
- HY-U00207
-
-
- HY-P0209
-
-
- HY-112604
-
-
- HY-112703
-
-
- HY-110037
-
-
- HY-G0012
-
-
- HY-108458
-
-
- HY-109074
-
-
- HY-143518
-
-
- HY-142868
-
-
- HY-101164
-
-
- HY-136842
-
-
- HY-123744
-
-
- HY-120277
-
-
- HY-A0229A
-
-
- HY-103335
-
-
- HY-169139
-
-
- HY-134125
-
-
- HY-125970
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
CRTh2 antagonist 2 is selective and potent CRTH2 antagonist extracted from patent US20140148470A1, compound Example 1, has an IC50 of ≤10 nM. CRTh2 antagonist 2 can be used in research of androgenic alopecia .
|
-
- HY-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-19818A
-
-
- HY-139681
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.
|
-
- HY-139680
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multitarget bitopic ligand (Ki = 1.58 nM) potentially useful for central nervous system disorders.
|
-
- HY-14825
-
|
SVT-40776
|
mAChR
|
Neurological Disease
|
|
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-120927
-
|
|
Others
|
Neurological Disease
|
|
Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development .
|
-
- HY-136459
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease .
|
-
- HY-161914
-
|
|
P2X Receptor
|
Neurological Disease
|
|
P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model .
|
-
- HY-14129
-
-
- HY-11103
-
-
- HY-10259A
-
-
- HY-10259
-
-
- HY-101407
-
-
- HY-13004
-
-
- HY-13796
-
-
- HY-15853
-
-
- HY-107765
-
-
- HY-103533
-
-
- HY-14770
-
-
- HY-G0011
-
-
- HY-50669
-
-
- HY-103408
-
-
- HY-107672
-
|
Stilonium iodide
|
nAChR
|
Neurological Disease
|
|
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM .
|
-
- HY-103495
-
-
- HY-155879
-
-
- HY-P2669
-
-
- HY-147543
-
-
- HY-147544
-
-
- HY-147545
-
-
- HY-16978
-
-
- HY-155300
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease .
|
-
- HY-146457
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations .
|
-
- HY-163274
-
-
- HY-12870
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).
|
-
- HY-12870A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-162011
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
|
-
- HY-16346S
-
-
- HY-U00353
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
Endocrinology
|
|
MCHR1 antagonist 1 is a selective antagonist of melanin concentrating hormone-1 (MCH1) receptor, with a Kb of 1 nM and a Ki of 4 nM at human MCH1, and may be used to reduce the body mass.
|
-
- HY-107603
-
|
|
iGluR
|
Neurological Disease
|
|
NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors .
|
-
- HY-155490
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
|
Cancer
|
|
Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KD SPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells .
|
-
- HY-10052
-
-
- HY-15403A
-
-
- HY-17001A
-
-
- HY-50669A
-
-
- HY-U00253
-
-
- HY-100471
-
-
- HY-10560
-
-
- HY-19391
-
-
- HY-19193
-
-
- HY-19654
-
-
- HY-117793
-
-
- HY-108972
-
-
- HY-109718
-
-
- HY-104061
-
|
|
TRP Channel
|
Others
|
|
AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM .
|
-
- HY-104062
-
|
|
TRP Channel
|
Others
|
|
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM .
|
-
- HY-107749
-
-
- HY-13209C
-
-
- HY-110132
-
-
- HY-105436
-
-
- HY-111295
-
|
|
Adenosine Receptor
|
Others
|
LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM .
|
-
- HY-P1681
-
-
- HY-106397A
-
-
- HY-106397
-
-
- HY-128544A
-
-
- HY-117256
-
-
- HY-12371
-
|
|
mGluR
|
Neurological Disease
|
|
VU0431316 is a potent and selective non-competitive antagonist of mGlu5 with an IC50 value of 24 nM .
|
-
- HY-123757
-
-
- HY-B1613
-
-
- HY-10560A
-
-
- HY-14339
-
|
SB-742457; GSK-742457; RVT-101
|
5-HT Receptor
|
Neurological Disease
|
|
Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.
|
-
- HY-16578
-
GW9662
Maximum Cited Publications
139 Publications Verification
|
PPAR
|
Cancer
|
|
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
|
-
- HY-10871
-
|
CP-945598
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
|
-
- HY-10871A
-
|
CP 945598 Hydrochloride
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
|
-
- HY-10815
-
|
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-120792
-
|
|
Others
|
Others
|
|
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
|
-
- HY-162408
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
|
-
- HY-162409
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
|
-
- HY-13232
-
|
|
Itk
|
Inflammation/Immunology
|
|
ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM .
|
-
- HY-157495
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC50 of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats .
|
-
- HY-168098
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y6R antagonist 1 (compound 5ab) is a selective, orally active P2Y6R antagonist with an IC50 value of 19.6 nM. P2Y6R antagonist 1 has anti-inflammatory activity .
|
-
- HY-14277AR
-
|
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (hydrochloride) (Standard) is the analytical standard of Levocabastine (hydrochloride). This product is intended for research and analytical applications. Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-146436
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 2 (compound 6) is a potent AT1R selective ligand. AT1R antagonist 2 exhibits a fair AT1R affinity, with a Ki of 26 nM .
|
-
- HY-N2304A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
|
-
- HY-134542
-
|
|
Calcium Channel
|
Neurological Disease
|
|
CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research .
|
-
- HY-107568
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM) .
|
-
- HY-117139
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor .
|
-
- HY-19658
-
-
- HY-U00084
-
-
- HY-19110
-
-
- HY-19274
-
-
- HY-15195
-
-
- HY-10634
-
-
- HY-15835
-
|
GDC-0917
|
IAP
|
Cancer
|
|
CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
|
-
- HY-12635
-
-
- HY-19768
-
-
- HY-19736
-
-
- HY-15411
-
-
- HY-U00251
-
-
- HY-111398
-
-
- HY-W018061
-
|
CP101,606
|
iGluR
|
Neurological Disease
|
|
Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
|
-
- HY-112629
-
-
- HY-100318
-
-
- HY-120689
-
-
- HY-101259
-
|
BMS 614
|
RAR/RXR
|
Cancer
|
|
BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a Ki of 2.5 nM .
|
-
- HY-142214
-
|
|
TRP Channel
|
Others
|
|
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
|
-
- HY-142658
-
|
|
Prostaglandin Receptor
|
Others
|
|
BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
|
-
- HY-76511
-
-
- HY-103363
-
-
- HY-103189
-
-
- HY-133178
-
|
|
Ephrin Receptor
|
Cancer
|
|
Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity .
|
-
- HY-142658A
-
|
|
Prostaglandin Receptor
|
Others
|
|
BAY-6672 hydrochloride is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
|
-
- HY-107696
-
-
- HY-W018061A
-
|
CP101,606 mesylate
|
iGluR
|
Neurological Disease
|
|
Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
|
-
- HY-135501
-
-
- HY-118420
-
|
|
RAR/RXR
|
Cancer
|
|
BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM .
|
-
- HY-A0229
-
|
GR 138950
|
Others
|
Others
|
|
Saprisartan (GR 138950) is a selective, long-acting AT1 receptor antagonist with low receptor dissociation kinetics.
|
-
- HY-101542
-
-
- HY-123142
-
-
- HY-121453
-
-
- HY-105018A
-
|
GSK 557296 benzenesulfonate
|
Oxytocin Receptor
|
Others
|
|
Epelsiban Besylate (GSK 557296 benzenesulfonate) is an orally active compound known for its highly selective oxytocin receptor antagonist.
|
-
- HY-144764
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT1A antagonist 1 (compound 6f) is a potent and selective antagonist of 5-HT1A receptor, with a Ki of 35 nM. 5-HT1A antagonist 1 can be used for the research of CNS diseases .
|
-
- HY-163895
-
|
|
Fluorescent Dye
Opioid Receptor
|
Neurological Disease
|
|
δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
|
-
- HY-112340
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects .
|
-
- HY-114191B
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM) .
|
-
- HY-146431
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 1 (compound 10) is a potent AT1R selective ligand. AT1R antagonist 1 exhibits a fair AT1R affinity, with a Ki of 8.5 nM .
|
-
- HY-150693
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively .
|
-
- HY-157936
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
|
-
- HY-146456
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases .
|
-
- HY-14825A
-
|
SVT-40776 D-tartrate
|
mAChR
|
Neurological Disease
|
|
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-102037
-
-
- HY-100798
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .
|
-
- HY-12131
-
-
- HY-10486
-
-
- HY-17024
-
|
11-Deoxojervine
|
Hedgehog
Smo
Endogenous Metabolite
|
Cancer
|
|
Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
|
-
- HY-12301
-
-
- HY-18966
-
-
- HY-19347
-
|
WD-Repeat Protein 5-0103
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
|
-
- HY-12777
-
-
- HY-U00143
-
-
- HY-101105A
-
-
- HY-15068
-
|
FG9202
|
iGluR
|
Neurological Disease
|
|
NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity .
|
-
- HY-114025
-
-
- HY-118678
-
-
- HY-120090
-
-
- HY-128351
-
-
- HY-16756
-
-
- HY-105018
-
|
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-104059
-
-
- HY-A0252
-
-
- HY-107679
-
-
- HY-102095
-
|
|
mGluR
|
Neurological Disease
|
|
SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM .
|
-
- HY-150138
-
|
GV 150526
|
iGluR
|
Neurological Disease
|
|
Gavestinel (GV 150526) is a selective and potent the glycine site of the NMDA receptor antagonist. Gavestinel has neuroprotectant effects .
|
-
- HY-118546
-
-
- HY-101262
-
-
- HY-120192
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms .
|
-
- HY-116309
-
-
- HY-105332
-
|
|
CRFR
|
Neurological Disease
|
|
CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties .
|
-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis .
|
-
- HY-162661
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis .
|
-
- HY-144733
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
|
-
- HY-144610
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .
|
-
- HY-128063
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes) .
|
-
- HY-103104
-
|
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
|
-
- HY-144609
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
|
-
- HY-144608
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
|
-
- HY-103134
-
|
|
Others
|
Inflammation/Immunology
|
|
5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT4) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT4 receptor .
|
-
- HY-15577
-
|
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-15084
-
|
(+)-MK 801 Maleate
|
iGluR
|
Neurological Disease
|
|
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
|
-
- HY-A0024
-
|
(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
|
mAChR
|
Neurological Disease
Cancer
|
|
Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-100717
-
-
- HY-14130
-
-
- HY-111484
-
|
SRN-927
|
Estrogen Receptor/ERR
|
Cancer
|
|
GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist .
|
-
- HY-112895
-
UT-155
2 Publications Verification
|
Androgen Receptor
|
Cancer
|
|
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
|
-
- HY-111442
-
-
- HY-110255
-
|
|
mGluR
|
Neurological Disease
|
|
AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 has antinociception effects .
|
-
- HY-107735
-
-
- HY-N1163
-
-
- HY-P1017
-
-
- HY-15726
-
-
- HY-110255A
-
|
|
mGluR
|
Neurological Disease
|
|
AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects .
|
-
- HY-P1726
-
-
- HY-103126
-
-
- HY-17037S
-
-
- HY-107699
-
|
|
iGluR
|
Neurological Disease
|
|
PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors .
|
-
- HY-101139
-
-
- HY-101139A
-
|
XAC hydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice .
|
-
- HY-12710
-
|
α-Yohimbine; Corynanthidine; Isoyohimbine
|
Adrenergic Receptor
|
Cancer
|
|
Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
|
-
- HY-19654C
-
|
(1S,5R)-GSK598809 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist.
|
-
- HY-101105
-
-
- HY-106356
-
-
- HY-103379
-
-
- HY-117040
-
|
Norbinaltorphimine; NorBNI
|
Opioid Receptor
|
Others
|
|
nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo .
|
-
- HY-115273
-
|
|
P2Y Receptor
|
Others
|
|
MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with KB of 0.177 μM .
|
-
- HY-106769
-
-
- HY-123182
-
-
- HY-106769C
-
|
GR50360 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent .
|
-
- HY-144137
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .
|
-
- HY-15472
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
|
-
- HY-15472A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
|
-
- HY-108432
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-741672 is a selective and orally active CCR2 antagonist with an IC50 of 1.1 nM. BMS-741672 shows >700-fold selective for CCR2 than CCR5 .
|
-
- HY-159896
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 8 (Compound 20f) is an effective, orally active, and selective PAR4 antagonist with an IC50 value of 15.32 nM. PAR4 antagonist 8 exhibits favorable pharmacokinetic properties. PAR4 antagonist 8 not only effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50 = 6.39 nM) but also inhibits mouse platelet aggregation. PAR4 antagonist 8 can be used in antithrombotic research .
|
-
- HY-114191
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-114191A
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-121186
-
-
- HY-157453
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC50 of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC50: 0.007 μM) and Ca 2+ mobilization (IC50: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research .
|
-
- HY-125819
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .
|
-
- HY-101598
-
-
- HY-10888
-
|
KW-6002
|
Adenosine Receptor
|
Neurological Disease
|
|
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
|
-
- HY-15481
-
-
- HY-100407
-
|
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-12488
-
|
|
CXCR
|
Endocrinology
Cancer
|
|
LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
|
-
- HY-U00237
-
-
- HY-101395
-
-
- HY-14551
-
|
SR142801
|
Neurokinin Receptor
|
Neurological Disease
|
|
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia .
|
-
- HY-112248
-
-
- HY-15853A
-
-
- HY-103516
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research .
|
-
- HY-103153
-
-
- HY-142617
-
-
- HY-A0249
-
-
- HY-116263
-
-
- HY-111082
-
|
|
Adenosine Receptor
|
Others
|
|
ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM .
|
-
- HY-18345
-
-
- HY-146134
-
-
- HY-105014
-
|
Norastemizole
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities .
|
-
- HY-13710A
-
-
- HY-P1194B
-
-
![[D-Pro2] Spantide I TFA](//file.medchemexpress.eu/product_pic/hy-p1194b.gif)
- HY-121394
-
-
- HY-108667
-
|
|
P2X Receptor
|
Others
|
|
TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats .
|
-
- HY-100797
-
|
(±)-CPP
|
iGluR
|
Neurological Disease
|
|
(RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity .
|
-
- HY-109036
-
-
- HY-P3227
-
|
XJ735
|
Integrin
|
Inflammation/Immunology
|
|
Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertension
Research .
|
-
- HY-103116
-
-
- HY-117557
-
-
- HY-105798
-
-
- HY-13209R
-
-
- HY-105275A
-
-
- HY-125087
-
-
- HY-111037
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-457 is a potent and selective CCR1 antagonist. BMS-457 can be used in the study of rheumatoid arthritis .
|
-
- HY-167946
-
|
|
Others
|
Others
|
|
CP-866087 is a new, highly effective, and selective antagonist of the mu-opioid receptor designed for exploring female sexual dysfunction.
|
-
- HY-158318
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NUDT5/14 antagonist 1 (Compound 9) is a selective, dual antagonist for nucleotide diphosphate kinase NUDT5 and NUDT14, with IC50 of 0.27 and 0.16 μM, respectively. NUDT5/14 antagonist 1 binds to Bruton’s tyrosine kinase (BTK) with an IC50 of 0.377 μM .
|
-
- HY-111501
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
|
-
- HY-W471937
-
-
- HY-108513
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .
|
-
- HY-13706A
-
|
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model .
|
-
- HY-100405
-
|
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1 .
|
-
- HY-N9141
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica .
|
-
- HY-101337
-
-
- HY-12127
-
-
- HY-16582A
-
|
Erismodegib; LDE225; NVP-LDE225
|
Smo
|
Cancer
|
|
Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
|
-
- HY-15488A
-
-
- HY-15488
-
-
- HY-15653
-
-
- HY-10388
-
-
- HY-101833
-
-
- HY-B1541
-
-
- HY-103449
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM .
|
-
- HY-15068A
-
|
FG9202 disodium
|
iGluR
|
Neurological Disease
|
|
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity .
|
-
- HY-19361
-
-
- HY-139310
-
|
|
LPL Receptor
|
Others
|
|
GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis .
|
-
- HY-103376
-
|
|
CRFR
|
Neurological Disease
|
|
NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM .
|
-
- HY-101395A
-
-
- HY-101356
-
|
|
mGluR
|
Neurological Disease
|
|
CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
|
-
- HY-101375
-
|
|
mGluR
|
Neurological Disease
|
|
(RS)-APICA is a selective group II metabotropic glutamate receptor (mGluR II) antagonist. (RS)-APICA shows potential neuroprotective effect .
|
-
- HY-141711
-
|
|
mAChR
|
Neurological Disease
|
|
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4 .
|
-
- HY-100913
-
-
- HY-110292
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
A-425619, a potent and selective TRPV1 receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain .
|
-
- HY-100945
-
|
|
mAChR
|
Neurological Disease
|
|
Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (Ki: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers .
|
-
- HY-101337A
-
|
RS 21361
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research .
|
-
- HY-118450
-
-
- HY-N6097
-
-
- HY-101352
-
-
- HY-118904
-
-
- HY-150692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-111616
-
|
|
PPAR
Angiotensin Receptor
|
Cardiovascular Disease
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-12080
-
|
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-116213
-
-
- HY-135608
-
|
|
Others
|
Others
|
|
BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.
|
-
- HY-144607
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
|
-
- HY-118638
-
-
- HY-50175
-
-
- HY-15676
-
|
RG7388
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
|
-
- HY-100129
-
|
|
TRP Channel
|
Neurological Disease
|
|
JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine .
|
-
- HY-100409
-
|
|
mGluR
|
Cancer
|
|
PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect .
|
-
- HY-12525
-
|
|
GCGR
|
Metabolic Disease
|
|
LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research .
|
-
- HY-101910
-
|
N-(p-Methylphenylsulfonyl)phenoxazine
|
P2X Receptor
|
Neurological Disease
|
|
PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
|
-
- HY-100720
-
-
- HY-P1276
-
|
Neurokinin-2 receptor antagonist
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
|
-
- HY-112202
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4 .
|
-
- HY-101226
-
|
|
mGluR
|
Neurological Disease
|
|
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
|
-
- HY-107437
-
|
|
RAR/RXR
|
Metabolic Disease
|
|
CD2665 is an orally active and selective RAR-β,γ antagonist, with Kd values of 306 nM, 110 nM for RAR-β and RAR-γ, repectively .
|
-
- HY-13505
-
-
- HY-19477
-
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-137442
-
|
EOS-850
|
Adenosine Receptor
|
Cancer
|
|
Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity .
|
-
- HY-B0298AS
-
-
- HY-107326
-
-
- HY-50175A
-
-
- HY-119868
-
|
Butoxamin
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity .
|
-
- HY-137180
-
-
- HY-107326A
-
-
- HY-120867
-
-
- HY-103557
-
|
|
mGluR
|
Neurological Disease
|
|
Ro 64-5229 is a selective, non-competitive mGlu2 antagonist. RO 64-5229 reduces the presynaptic inhibitory effect of Neuroligin 1 .
|
-
- HY-153152
-
-
- HY-15402D
-
|
BMS 207940 hydrate
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
|
-
- HY-107693
-
-
- HY-148656
-
-
- HY-14230
-
|
|
CCR
HIV
|
Infection
|
|
INCB9471 is a potent, selective and orally active CCR5 antagonist. INCB9471 shows anti-HIV-1 activity .
|
-
- HY-103143A
-
-
- HY-123869
-
-
- HY-107567B
-
|
β-Alanylhistamine dihydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Carcinine (β-Alanylhistamine) dihydrochloride is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .
|
-
- HY-117216
-
-
- HY-103143
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SDZ 205-557 hydrochloride is a selective 5-HT4 receptors antagonist. SDZ 205-557 hydrochloride can be used for neurological research .
|
-
- HY-12525A
-
|
|
GCGR
|
Metabolic Disease
|
|
LGD-6972 sodium is a selective and orally active glucagon receptor antagonist. LGD-6972 sodium has the potential for type 2 diabetes research .
|
-
- HY-12080A
-
|
ZK-811752 hydrochloride
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-10896
-
-
- HY-147506
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs .
|
-
- HY-125820
-
|
|
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .
|
-
- HY-146410
-
|
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
|
-
- HY-127024
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
|
-
- HY-162787
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
|
-
- HY-B0569
-
|
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
|
-
- HY-148350
-
|
|
PTHR
|
Cancer
|
|
DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM. DS69910557 can be used for the research of hyperparathyroidism, hypercalcemia of malignancy and osteoporosis .
|
-
- HY-161273
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .
|
-
- HY-121383
-
|
AH5158; Sch-15719W free base
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-107606
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine .
|
-
- HY-19431
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
|
-
- HY-107606A
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ～30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine .
|
-
- HY-107567
-
|
β-Alanylhistamine
|
Histamine Receptor
|
Neurological Disease
|
|
Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .
|
-
- HY-13274
-
-
- HY-10633
-
|
|
TRP Channel
|
Neurological Disease
|
|
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
|
-
- HY-16582
-
|
Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate
|
Smo
|
Cancer
|
|
Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
|
-
- HY-12497
-
|
|
Trk Receptor
|
Neurological Disease
|
|
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.
|
-
- HY-12503
-
CFM-2
1 Publications Verification
|
iGluR
|
Neurological Disease
Cancer
|
|
CFM-2 is a potent and selective non-competitive AMPAR antagonist . CFM-2 possesses anticonvulsant activity in various models of seizures .
|
-
- HY-19532
-
-
- HY-14791A
-
|
(±)-SLV319; (±)-BMS-646256
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
(±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
|
-
- HY-U00185
-
-
- HY-107382
-
-
- HY-119433
-
|
J867
|
Progesterone Receptor
|
Endocrinology
|
|
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human .
|
-
- HY-135588
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis .
|
-
- HY-115506
-
|
|
TRP Channel
|
Neurological Disease
|
|
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain .
|
-
- HY-16683
-
|
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.
|
-
- HY-107382A
-
-
- HY-136462
-
|
|
LPL Receptor
|
Infection
|
|
CYM50358 is a potent and selective S1PR4 antagonist, with an IC50 of 25 nM. CYM50358 can be used for the research of influenza infection .
|
-
- HY-131914A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain .
|
-
- HY-101378
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 54626 (hydrochloride) is a selective antagonist of GABAB receptor with an IC50 value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABAB receptors in neurological signaling .
|
-
- HY-44154
-
|
|
Others
|
Metabolic Disease
|
|
PSB-CB5 is a potent and selective antagonist of GRP18. PSB-CB5 has the potential for the research of metabolic disease and obesity .
|
-
- HY-107733
-
-
- HY-150124
-
|
|
Integrin
|
Cancer
|
|
K34c is a potent and selective α5β1 integrin antagonist. K34c can be used for glioblastoma research .
|
-
- HY-13710
-
-
- HY-101367A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR 55562 dihydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 dihydrochloride can be used for the research of nerve disease .
|
-
- HY-149290
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity .
|
-
- HY-W010869
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR 55562 hydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 hydrochloride can be used for the research of nerve disease .
|
-
- HY-14778A
-
|
(S)-GSK 221149; (S)-GSK 221149A
|
Others
|
Neurological Disease
Endocrinology
|
|
(S)-Retosiban is the isomer of Retosiban (HY-14778), and can be used as an experimental control. Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a Ki of 0.65 nM.
|
-
- HY-P3213
-
-
![Dp[Tyr(methyl)2,Arg8]-Vasopressin](//file.medchemexpress.eu/product_pic/hy-p3213.gif)
- HY-110270
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
RN-9893 is a potent and selective TRPV4 receptor antagonist with IC50 values of 320, 420 and 660 nM for mouse, human and rat channels, respectively .
|
-
- HY-100821
-
|
|
Bacterial
|
Infection
|
|
2,4-Dihydroxyphenylacetylasparagine is a potent and selective antagonist of glutamate. 2,4-Dihydroxyphenylacetylasparagine inhibits glutamate binding to rat brain synaptic membranes .
|
-
- HY-120386
-
|
|
iGluR
|
Neurological Disease
|
|
LY382884 is a selective antagonist for GluR5 kainate receptor. LY382884 prevents the induction of NMDA receptor independent long-term potentiation (LTP) .
|
-
- HY-162556
-
|
(+)-dmXeB
|
Apoptosis
|
Cancer
|
|
(+)-Desmethylxestospongin B ((+)-dmXeB) is a potent antagonist of inositol triphosphate receptor (IP3R), leading to cellular autophagy and allowing selective tumor cell apoptosis .
|
-
- HY-117216A
-
-
- HY-117216B
-
-
- HY-B1277A
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
|
-
- HY-B1397
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-B1397A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine dihydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine dihydrochloride can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-B1397C
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine hydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine hydrochloride can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-123106
-
|
|
Others
|
Others
|
|
MCL-0129 is a compound with anxiolytic and antidepressant activity and is a selective MC4 receptor antagonist that exhibits anxiolytic and antidepressant-like behaviors in multiple rodent models.
|
-
- HY-144606
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
|
-
- HY-161247
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
|
-
- HY-131337
-
|
|
Bacterial
|
Infection
|
|
RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections . RhlR antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15370A
-
|
SB-269970A
|
5-HT Receptor
|
Neurological Disease
|
|
SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors .
|
-
- HY-15370
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors .
|
-
- HY-P1278
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-P1278A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-107559
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
|
-
- HY-101355A
-
-
- HY-18971
-
TG4-155
1 Publications Verification
|
Prostaglandin Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM . TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1 . TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor .
|
-
- HY-114452
-
|
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
|
-
- HY-19638A
-
|
AR-C69931MX tetrasodium
|
P2Y Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist .
|
-
- HY-U00076
-
-
- HY-10889
-
|
SCH-420814
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
|
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
|
-
- HY-13331
-
|
Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-16711
-
-
- HY-19904
-
|
LY2409021
|
GCGR
|
Metabolic Disease
|
|
Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus .
|
-
- HY-100454
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
CGP 25454A is a selective presynaptic dopamine autoreceptor antagonist which induces the increase of dopamine and acetyl choline. CGP 25454A can be used for major depression research .
|
-
- HY-101736
-
AMG9810
4 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
|
-
- HY-U00104
-
|
|
mAChR
|
Endocrinology
|
|
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
|
-
- HY-U00355
-
-
- HY-101978
-
|
CPI-444; V81444
|
Adenosine Receptor
|
Cancer
|
|
Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses .
|
-
- HY-13466
-
-
- HY-19902
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents .
|
-
- HY-P1276A
-
|
Neurokinin-2 receptor antagonist TFA
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor .
|
-
- HY-120261
-
-
- HY-N2064
-
|
|
mAChR
|
Neurological Disease
|
|
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control .
|
-
- HY-107649
-
|
UK-76654 fumarate
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome .
|
-
- HY-123337
-
|
UK-76654
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome .
|
-
- HY-133555
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
|
-
- HY-131278
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Olmesartan methyl ester is an intermediate in the synthesis of Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor antagonist with IC50 of 66.2 μM .
|
-
- HY-P1233
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit .
|
-
- HY-B1789A
-
|
|
mAChR
|
Neurological Disease
|
|
Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects .
|
-
- HY-119802
-
-
- HY-101924
-
-
- HY-101473
-
|
|
Integrin
|
Inflammation/Immunology
|
|
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research .
|
-
- HY-135542
-
|
|
CRFR
|
Others
|
|
NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily .
|
-
- HY-110179
-
-
- HY-107713
-
|
|
iGluR
|
Neurological Disease
|
|
PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D containing receptors .
|
-
- HY-129030
-
|
|
iGluR
|
Neurological Disease
|
|
BDZ-g is a potent, selective antagonist of AMPA receptor. BDZ-g has the potential for the research of various neurological disorders involving excessive activity of AMPA receptors .
|
-
- HY-121616
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
(R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319
|
-
- HY-109022
-
|
MK-8031; AGN-241689
|
CGRP Receptor
|
Neurological Disease
|
|
Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine .
|
-
- HY-14551B
-
|
(S)-SR142801
|
Neurotensin Receptor
|
Neurological Disease
|
|
(S)-Osanetant is the S-enantiomer of Osanetant. Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia .
|
-
- HY-129810
-
-
- HY-101373A
-
|
SKF 95282 dimaleate
|
Histamine Receptor
|
Neurological Disease
|
|
Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception .
|
-
- HY-129826
-
|
|
mAChR
|
Others
|
|
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
|
-
- HY-160440A
-
|
|
mAChR
|
Neurological Disease
|
|
VU6021625 is a selective antagonist muscarinic acetylcholine receptors (mAChRs), with the IC50 value of 0.44 nM, 57 nM for human M4 and rat M4, respectively .
|
-
- HY-119739
-
|
|
GCGR
|
Metabolic Disease
Cancer
|
|
Skyrin is an anthraquinone compound that can be isolated from almond fruit. Skyrin is a receptor-selective glucagon antagonist. Skyrin can inhibit the growth of tumor cells .
|
-
- HY-B1277
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
|
-
- HY-118232
-
-
- HY-124392
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
AMG580 is a selective PDE10A antagonist with subnanomolar affinity for rat, primate, and human PDE10A. AMG580 can be used for the research of noninvasive radiotracer .
|
-
- HY-121720
-
-
- HY-103164A
-
|
CSC
|
Others
|
Neurological Disease
|
|
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitory activity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .
|
-
- HY-133123
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors .
|
-
- HY-161405
-
|
|
Neuropeptide FF Receptor
Opioid Receptor
|
Neurological Disease
|
|
NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively .
|
-
- HY-76612
-
-
- HY-108229
-
|
6β-Hydroxynaltrexone
|
Drug Metabolite
Opioid Receptor
|
Neurological Disease
|
|
6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
|
-
- HY-B1517B
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Alprenolol benzoate is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol benzoate is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
|
-
- HY-113960
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1 .
|
-
- HY-101199
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .
|
-
- HY-101724
-
|
NNC-05-1869 hydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
|
-
- HY-101355B
-
|
CGP 20712 mesylate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
-
- HY-12130
-
|
|
CRFR
|
Neurological Disease
|
|
CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities .
|
-
- HY-12129
-
|
|
CFTR
|
Neurological Disease
|
|
CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 hydrochloride has anxiolytic activities .
|
-
- HY-13245
-
|
INCB8761
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-15418
-
|
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
|
-
- HY-12381
-
ML224
1 Publications Verification
NCGC00242364; ANTAG3
|
TSH Receptor
|
Endocrinology
|
|
ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.
|
-
- HY-16996A
-
|
|
Sigma Receptor
|
Neurological Disease
|
BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia .
|
-
- HY-90010
-
|
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
Cancer
|
|
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-12981
-
-
- HY-11029
-
-
- HY-14447S
-
-
- HY-111271A
-
-
- HY-112284
-
|
OBE022
|
Prostaglandin Receptor
|
Endocrinology
|
|
Ebopiprant (OBE022) is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.
|
-
- HY-76511S
-
|
MK-679-d6; L 668019-d6
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
|
-
- HY-101336
-
-
- HY-14121
-
-
- HY-120691A
-
-
- HY-117819
-
|
|
ROR
|
Inflammation/Immunology
|
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM .
|
-
- HY-16682
-
|
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
|
-
- HY-10388A
-
|
|
Calcium Channel
|
Others
|
|
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca 2+ channel antagonist.
|
-
- HY-109170
-
|
BAY 1817080
|
P2X Receptor
|
Inflammation/Immunology
|
|
Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough .
|
-
- HY-101223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .
|
-
- HY-103357
-
-
- HY-145234
-
-
- HY-138937
-
|
|
FXR
|
Metabolic Disease
|
|
NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research .
|
-
- HY-101241
-
|
|
mGluR
|
Neurological Disease
|
|
MPPG is a potent and selective L-AP4-sensitive receptor antagonist with an kD value of 9.2 μM, being tested on the neonatal rat spinal cord .
|
-
- HY-17495
-
-
- HY-P1628
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea .
|
-
- HY-107748
-
|
5'-GNTI hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor .
|
-
- HY-110107
-
-
- HY-P1442
-
|
|
Adrenergic Receptor
|
Cancer
|
|
AdTx1 is a selective α1A-adrenoceptor antagonist (Ki: 0.35 nM). AdTx1 can be used for research of benign prostatic hyperplasia .
|
-
- HY-120188
-
|
|
PPAR
|
Others
|
|
CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
|
-
- HY-137442A
-
|
EOS-850 hydrochloride
|
Adenosine Receptor
|
Cancer
|
|
Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. Inupadenant hydrochloride is not brain-penetrant. Inupadenant hydrochloride has potent anti-tumor activity .
|
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-122230
-
|
|
Integrin
|
Cardiovascular Disease
|
|
UR-3216 is a selective, and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 has the potential for cardiovascular diseases research .
|
-
- HY-101986C
-
|
AR-H 053591 dihydrochloride
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 value of 15 nM .
|
-
- HY-119095
-
-
- HY-B1397B
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine lactate, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine lactate can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-112284A
-
|
OBE022 hydrochloride
|
Prostaglandin Receptor
|
Endocrinology
|
|
Ebopiprant (OBE022) hydrochloride is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.
|
-
- HY-107723A
-
|
|
Others
|
Metabolic Disease
|
|
CGP 71683 Free base serves as a powerful and highly selective non-peptide antagonist targeting the NPY Y(5) receptor, making it a valuable tool in obesity research.
|
-
- HY-13004R
-
|
|
CCR
HIV
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Maraviroc (Standard) is the analytical standard of Maraviroc. This product is intended for research and analytical applications. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
|
-
- HY-125821
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .
|
-
- HY-146808
-
|
|
Galectin
|
Cancer
|
|
Galectin-3 antagonist 1 (compound 15) is a potent and selective Galectin-3 (Gal-3) antagonist with Kd value of 5.3 μM. Meanwhile, Galectin-3 antagonist 1 binds to various Galectin with Kd values of 250 μM (Gal-4N), 18 μM (Gal-4C), 450 μM (Gal-8C), respectively .
|
-
- HY-10898
-
-
- HY-101980
-
|
HTL1071; AZD4635
|
Adenosine Receptor
|
Cancer
|
|
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors .
|
-
- HY-100607A
-
|
ONO1101 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist .
|
-
- HY-101382
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GR 103691 is a potent, selective dopamine D3 receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites .
|
-
- HY-12436
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM) .
|
-
- HY-100607
-
-
- HY-B1517
-
|
(RS)-Alprenolol; dl-Alprenolol
|
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
|
-
- HY-B1517A
-
|
(RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride
|
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
|
-
- HY-115487
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research .
|
-
- HY-144138
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .
|
-
- HY-19638
-
|
AR-C69931MX
|
P2Y Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist .
|
-
- HY-121186R
-
|
|
Adrenergic Receptor
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
|
Bevantolol (hydrochloride) (Standard) is the analytical standard of Bevantolol (hydrochloride). This product is intended for research and analytical applications. Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
|
-
- HY-117799
-
|
|
5-HT Receptor
|
Endocrinology
|
|
LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
|
-
- HY-15894
-
-
- HY-17503
-
-
- HY-15950
-
-
- HY-108329
-
-
- HY-108463
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-117965
-
-
- HY-128878
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
|
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist . Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8) .
|
-
- HY-121599
-
|
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression .
|
-
- HY-P0062
-
-
- HY-101381
-
|
AF-DX 116
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
|
-
- HY-P1233A
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
ANQ-11125 TFA is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 TFA blocks motilide-induced contractions in vitro in the rabbit .
|
-
- HY-P0062B
-
-
- HY-124830
-
|
|
Others
|
Cancer
|
|
SPA70 is a potent and selective antagonist of human pregnane X receptor (hPXR), with an IC50 of 540 nM (Ki=390 nM). SPA70 can enhance the chemosensitivity of cancer cells .
|
-
- HY-116569
-
-
- HY-107728
-
-
- HY-101347
-
|
|
nAChR
|
Neurological Disease
|
|
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way .
|
-
- HY-108479
-
|
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-124475
-
|
|
CRFR
|
Neurological Disease
|
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier .
|
-
- HY-122246
-
|
|
GPR55
PKC
ERK
Arrestin
|
Metabolic Disease
|
|
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
|
-
- HY-15023
-
|
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
|
Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
|
-
- HY-101349A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L 741742 hydrochloride is an orally active and selective antagonist of hD4 receptors. L 741742 hydrochloride has a good brain penetration. L 741742 hydrochloride can be used in study nervous system disorders, particularly schizophrenia .
|
-
- HY-149703
-
|
|
Others
|
Neurological Disease
|
|
M1/M4 muscarinic antagonist 2 (compound 40) is a selective M1 and M4 agonist with IC5019 nM and 42 nM, respectively .
|
-
- HY-12701A
-
|
U-99194A; PNU-99194A maleate; JPC-211 maleate
|
Dopamine Receptor
|
Neurological Disease
|
|
U-99194 maleate is a potent and selective Dopamine3 Receptor (D3 receptor) antagonist. U-99194 maleate also enhances prolactin secretion and striatal dopamine synthesis .
|
-
- HY-114674
-
-
- HY-16582AS
-
|
Erismodegib-d4; LDE225-d4; NVP-LDE225-d4
|
Isotope-Labeled Compounds
|
Others
|
|
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
|
-
- HY-138453
-
|
LPA1 receptor antagonist 2
|
LPL Receptor
|
Inflammation/Immunology
|
|
ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases .
|
-
- HY-109122
-
|
ACT-246475
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Selatogrel (ACT-246475) is a reversible and selective P2Y12 receptor antagonist which inhibits platelet aggregation with an IC50 of 8 nM. Selatogrel exhibits antithrombotic efficacy .
|
-
- HY-10052R
-
-
- HY-13274A
-
-
- HY-129660
-
-
- HY-17503D
-
-
- HY-131914
-
|
|
Sigma Receptor
|
|
|
EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain .
|
-
- HY-103064
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP sodium is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP sodium is an inhibitor of ADP-dependent platelet aggregation .
|
-
- HY-P4745
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .
|
-
- HY-115827
-
|
|
Others
|
Others
|
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-159942
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice .
|
-
- HY-15419
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-13406
-
TAK-779
2 Publications Verification
Takeda 779
|
CCR
HIV
CXCR
|
Infection
Inflammation/Immunology
Endocrinology
|
|
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
|
-
- HY-19533
-
|
|
Adenosine Receptor
|
Cancer
|
|
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively .
|
-
- HY-15419A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-16578S
-
|
|
Isotope-Labeled Compounds
PPAR
|
Cancer
|
|
GW9662-d5 is the deuterium labeled GW9662. GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively[1][2].
|
-
- HY-111304
-
-
- HY-50697
-
|
|
P2X Receptor
|
Neurological Disease
|
|
A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
|
-
- HY-B0068
-
|
Y-25130 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Azasetron (Y-25130) hydrochloride, a benzamide derivative, is a potent and selective 5-HT3 receptor antagonist. Azasetron is used in the study for Chemotherapy-induced nausea and vomiting (CINV) .
|
-
- HY-15443
-
-
- HY-17617
-
|
Z-360
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Nastorazepide (Z-360), selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity .
|
-
- HY-10562
-
-
- HY-12789
-
|
APD334
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
|
-
- HY-10806
-
-
- HY-13556A
-
|
LY353381 hydrochloride; SERM III hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
|
-
- HY-12190
-
-
- HY-17497S
-
-
- HY-16617
-
|
VU0424238
|
mGluR
|
Neurological Disease
|
|
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration .
|
-
- HY-14777
-
|
RGH-896
|
iGluR
|
Neurological Disease
|
|
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions .
|
-
- HY-103090
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM .
|
-
- HY-120478
-
|
|
LPL Receptor
|
Infection
|
|
ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively .
|
-
- HY-108136A
-
|
BIM-X hydrochloride; Ro31-8425 hydrochloride
|
PKC
CDK
|
Cardiovascular Disease
|
|
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM .
|
-
- HY-129059
-
|
NNC 756
|
Dopamine Receptor
|
Neurological Disease
|
|
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer .
|
-
- HY-101348
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
|
-
- HY-U00189
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
|
-
- HY-U00423
-
-
- HY-N0584A
-
|
6-Hydroxyhyoscyamine hydrobromide
|
mAChR
|
Inflammation/Immunology
Cancer
|
|
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
|
-
- HY-111308
-
-
- HY-12190A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
|
-
- HY-103090A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM .
|
-
- HY-119350B
-
|
RUC-4 dihydrochloride
|
Integrin
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) dihydrochloride is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban dihydrochloride can be used for the research of myocardial infarction (MI) .
|
-
- HY-112248A
-
-
- HY-119350
-
|
RUC-4
|
Integrin
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI) .
|
-
- HY-139581
-
|
SUVN-911 free base
|
nAChR
|
Neurological Disease
|
|
Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression .
|
-
- HY-107729
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects .
|
-
- HY-107610
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma .
|
-
- HY-123825
-
-
- HY-12717
-
|
|
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
|
-
- HY-101313
-
|
(-)-Remoxipride
|
Dopamine Receptor
|
Neurological Disease
|
|
(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder .
|
-
- HY-W025443
-
|
|
Others
|
Others
|
|
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist .
|
-
- HY-124740
-
|
|
Melanocortin Receptor
|
Cancer
|
|
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .
|
-
- HY-101313A
-
|
(-)-Remoxipride hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
(S)-Remoxipride ((-)-Remoxipride) hydrochloride is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride hydrochloride can be used for the research of psychotic disorder .
|
-
- HY-103208
-
|
|
Others
|
Metabolic Disease
|
|
Benalfocin is a novel selective alpha-2 adrenergic receptor antagonist. Benalfocin reduces blood pressure and heart rate. Benalfocin can be used in the study of cardiovascular effects .
|
-
- HY-110351
-
|
PGN 1531 hydrochloride
|
Prostaglandin Receptor
|
Neurological Disease
|
|
BGC 20-1531 (PGN 1531) hydrochloride is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC 20-1531 hydrochloride has the potential for the research of migraine headache .
|
-
- HY-P5833
-
|
κ-Bgt
|
nAChR
|
Neurological Disease
|
|
κ-Bungarotoxin (κ-Bgt) is a potent, selective, and slowly reversible antagonist of α3β2 neuronal nicotinic acetylcholine receptors with an IC50 of 2.30 nM .
|
-
- HY-123596
-
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
- HY-119350C
-
|
RUC-4 acetate
|
Integrin
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) acetate is a potent, selective platelet αIIbβ3antagonist (IC50=45 nM). Zalunfiban acetate can be used for the research of myocardial infarction (MI) .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-117880
-
|
CORT 125281
|
Glucocorticoid Receptor
|
Metabolic Disease
Endocrinology
|
|
Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM . Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia .
|
-
- HY-119389
-
-
- HY-121453R
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Bamifylline (hydrochloride) (Standard) is the analytical standard of Bamifylline (hydrochloride). This product is intended for research and analytical applications. Bamifylline hydrochloride is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist .
|
-
- HY-B0251
-
|
Epoxymexrenone
|
Mineralocorticoid Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV) .
|
-
- HY-116637
-
|
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
|
-
- HY-136172
-
ESI-08
1 Publications Verification
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .
|
-
- HY-101359
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-123038
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
CVT-5440 is a xanthine based, selective, high affinity A2B adenosine receptors (AdoR) antagonist with a Ki of 50 nM (selectivity A1> 200; A2A>200; A3>167). CVT-5440 has the potential for asthma research .
|
-
- HY-117799A
-
|
|
5-HT Receptor
|
Endocrinology
|
|
LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
|
-
- HY-119088
-
|
|
Others
|
Others
|
|
Estrogen receptor modulator 12 (compound 1a-(R)) is a selective estrogen receptor modulator with estrogen agonist and antagonist activities in in vivo models. Estrogen receptor modulator 12 exhibits antagonist effects on the uterus and estrogen agonist activities on bone, plasma lipids, hot flashes, and vagina in in vivo models, and is a potential compound for suppressing postmenopausal symptoms.
|
-
- HY-161727
-
|
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis .
|
-
- HY-116835
-
|
|
CCR
|
Inflammation/Immunology
|
|
BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research .
|
-
- HY-159578S
-
|
|
mAChR
|
Neurological Disease
|
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
- HY-116031
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
ATC0175 (free base) is a potent and selective antagonist of melanin-concentrating hormone receptor 1 (MCH-R1) with an IC50 value of 3.4 nM, as well as good selectivity over the Y5 and the α2A receptors. ATC0175 (free base) is promising for research of obesity .
|
-
- HY-119385
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
|
-
- HY-149854B
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 hydrochloride is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 hydrochloride has the effect of reducing mechanical hypersensitivity .
|
-
- HY-W721480
-
|
|
TRP Channel
|
Neurological Disease
|
|
HC-067047 hydrochloride is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .
|
-
- HY-12520B
-
|
(±)-SKF-38393 hydrochloride; SKF-38393A hydrochloride
|
Dopamine Receptor
Potassium Channel
|
Neurological Disease
|
|
(R)-SKF 38393 ((±)-SKF-38393) hydrochloride is a potent and selective D1 dopamine receptor antagonist. (R)-SKF 38393 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channel .
|
-
- HY-15072
-
|
YM 872
|
iGluR
|
Metabolic Disease
|
|
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
|
-
- HY-10302
-
|
|
CGRP Receptor
|
Neurological Disease
|
|
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
|
-
- HY-13955
-
-
- HY-17503B
-
-
- HY-B0321
-
|
Ro 1-7683
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
|
-
- HY-B0745
-
-
- HY-17503A
-
-
- HY-15069
-
|
ZK200775; MPQX
|
iGluR
|
Neurological Disease
|
|
Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-15069A
-
|
ZK200775 hydrate; MPQX hydrate
|
iGluR
|
Neurological Disease
|
|
Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-10794
-
-
- HY-100208
-
|
|
TRP Channel
|
Cancer
|
|
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .
|
-
- HY-115066
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents .
|
-
- HY-101784
-
|
|
GPR4
|
Inflammation/Immunology
|
|
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity .
|
-
- HY-135230
-
|
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
|
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
|
-
- HY-108908
-
-
- HY-105124A
-
|
Ro 3-4787 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-10309
-
|
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation .
|
-
- HY-19263
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
|
-
- HY-18970
-
-
- HY-103162
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease .
|
-
- HY-106612
-
|
U-K52046; Albanoquil
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research .
|
-
- HY-129250
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .
|
-
- HY-149854
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity .
|
-
- HY-108446
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT .
|
-
- HY-110001
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of 5-HT 1A (IC50=33.9 nM). (S)-WAY 100135 dihydrochloride has anxiolytic activity in animal models .
|
-
- HY-P1162
-
-
- HY-12191A
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
A 331440 hydrochloride is a histamine H3 receptor antagonist. A 331440 hydrochloride binds potently and selectively to human and rat histamine H3 receptors (Ki≤25 nM). A 331440 hydrochloride can be used for antiobesity research .
|
-
- HY-133732
-
|
GEA 654 hydrochloride; A03 hydrochloride
|
Serotonin Transporter
5-HT Receptor
iGluR
|
Neurological Disease
|
|
Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow .
|
-
- HY-153670
-
|
|
CCR
|
Cancer
|
|
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
|
-
- HY-107671
-
|
|
nAChR
|
Neurological Disease
|
|
DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .
|
-
- HY-A0252R
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
Bupranolol (Standard) is the analytical standard of Bupranolol. This product is intended for research and analytical applications. Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity .
|
-
- HY-19007
-
|
DA 4577
|
Histamine Receptor
|
Endocrinology
|
|
Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC50 3.28 μM .
|
-
- HY-12200
-
|
GSK189254
|
Histamine Receptor
|
Neurological Disease
|
|
GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively .
|
-
- HY-123499
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
|
|
SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .
|
-
- HY-17024R
-
|
|
Hedgehog
Smo
Endogenous Metabolite
|
Cancer
|
|
Cyclopamine (Standard) is the analytical standard of Cyclopamine. This product is intended for research and analytical applications. Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
|
-
- HY-123473
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-414796 is a selective, orally active and cross the blood-brain barrier dopamine D3 receptor antagonist with Ki values of 4, 400 nM for D3, D2, respectively .
|
-
- HY-103357A
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
LY262691 is a selective CCK-B antagonist with antipsychotic properties. LY262691 decreases the number of spontaneously active A9 and A10 dopamine cells and can be utilized in antipsychotic research .
|
-
- HY-111160
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF 83509, a desmethyl analogue of SCH 23390 (HY-19545A), is a selective dopamine D1 antagonist with a Ki of 70.2 nM. SKF 83509 has no activity at dopamine D2 receptors .
|
-
- HY-14575
-
|
Z-360 hemicalcium
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Nastorazepide (Z-360) hemicalcium, selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity .
|
-
- HY-18099A
-
|
E-52862 hydrochloride
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
|
-
- HY-107647
-
|
|
mAChR
Histamine Receptor
|
Inflammation/Immunology
|
|
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
- HY-114452A
-
|
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
|
-
- HY-103197
-
|
RX821002 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2) .
|
-
- HY-W795507
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
|
-
- HY-19904B
-
|
(+)-LY2409021
|
Others
|
Metabolic Disease
|
|
(+)-Adomeglivant ((+)-LY2409021) is a potent and selective glycogenotropin receptor antagonist with glucose-lowering activity. (+)-Adomeglivant reduces fasting blood glucose levels in both healthy subjects and patients with type 2 diabetes. The use of (+)-Adomeglivant can help investigate the mechanisms of hyperglycemia in type 2 diabetes. The antagonistic effect of (+)-Adomeglivant makes it challenging to assess the metabolic consequences of postprandial hyperglycemia .
|
-
- HY-107642
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility .
|
-
- HY-14791
-
|
SLV319; BMS-646256
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic .
|
-
- HY-107601
-
|
ACET
|
iGluR
|
Neurological Disease
|
|
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist .
|
-
- HY-111372A
-
|
(Rac)-BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .
|
-
- HY-121519
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels .
|
-
- HY-111191A
-
|
|
Others
|
Neurological Disease
|
|
(R)-ONO-2952 is a R-enantiomer of ONO-2952. ONO-2952 is a potent, selective and orally active TSPO antagonist with Kis of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes .
|
-
- HY-148252
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-116822
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM .
|
-
- HY-14137
-
|
SR 141716A Hydrochloride
|
Cannabinoid Receptor
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
|
-
- HY-13738A
-
|
Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
|
-
- HY-B0140
-
-
- HY-B0462A
-
-
- HY-15084A
-
|
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
|
-
- HY-14185
-
-
- HY-106441A
-
|
MK-0657; CERC-301
|
iGluR
|
Neurological Disease
|
|
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
|
-
- HY-107500
-
|
|
RAR/RXR
Autophagy
|
Others
|
|
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
|
-
- HY-101385
-
-
- HY-19654B
-
|
(1S,5R)-GSK598809
|
Dopamine Receptor
|
Others
|
|
(-)-GSK598809 ((1S,5R)-GSK598809) is an isomer of GSK598809. GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist.
|
-
- HY-123918
-
|
|
CX3CR1
|
Endocrinology
Cancer
|
|
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells .
|
-
- HY-115066A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents .
|
-
- HY-P0062A
-
-
- HY-135387
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
4-Desmethyl Istradefylline is a metabolite of Istradefylline. 4-Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease .
|
-
- HY-123918A
-
|
|
CX3CR1
|
Endocrinology
Cancer
|
|
JMS-17-2 hydrochloride is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 hydrochloride impairs metastatic seeding and colonization of breast cancer cells .
|
-
- HY-103406A
-
|
|
Dopamine Receptor
CCR
|
Neurological Disease
|
|
PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity .
|
-
- HY-19445
-
|
JB95008
|
Cholecystokinin Receptor
|
Cancer
|
|
Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer .
|
-
- HY-125989
-
|
2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation .
|
-
- HY-109171
-
-
- HY-N2005
-
-
- HY-108562
-
-
- HY-17503C
-
-
- HY-118388
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour .
|
-
- HY-103182
-
|
|
Adenosine Receptor
|
Others
|
|
PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) .
|
-
- HY-114072
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors .
|
-
- HY-W030796A
-
|
|
Taste Receptor
|
Metabolic Disease
|
|
Lactisole is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit, a glucose-sensing receptor. Lactisole inhibits insulin secretion induced by glucose in mouse islets .
|
-
- HY-103406
-
-
- HY-103182A
-
|
|
Adenosine Receptor
|
Others
|
|
PSB-1115 potassium salt is a selective A2B Adenosine Receptor antagonist. PSB-1115 potassium salt inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) .
|
-
- HY-110314
-
|
|
LPL Receptor
|
Infection
|
|
CYM50358 hydrochloride (compound 4v) is a potent, selective sphingosine-1-phosphate 4 (S1P4) receptor antagonist. CYM50358 hydrochloride can be used in the study of influenza infection .
|
-
- HY-101407R
-
-
- HY-123498
-
-
- HY-106246
-
|
EMD 281014 free acid; LY 2422347
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Pruvanserin (EMD 281014 free acid) is a selective 5-HT2A receptor antagonist. Pruvanserin alleviates tactile allodynia in diabetic rats. Pruvanserin can also be used for research of insomnia .
|
-
- HY-117636
-
|
|
Others
|
Others
|
|
(Rac)-L-659989 is the racemate of L-659989 (HY-121394). L-659989 s an orally active, extremely potent, selective and competitive platelet activating factor (PAF) receptor antagonist .
|
-
- HY-124911
-
|
|
5-HT Receptor
|
Infection
|
|
LY53857 free base is a selective 5-HT2 receptor antagonist with the ED50 of 17.5 nM. LY53857 free base shows antiviral activity against influenza A virus .
|
-
- HY-105537
-
|
RS-100975
|
Adrenergic Receptor
|
Endocrinology
|
|
Ro 70-0004 (RS-100975) is a selective alpha1A-adrenoceptor antagonist with a pKi of 8.9. Ro 70‐0004 can be used in the study of prostatic hyperplasia .
|
-
- HY-116773
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-69024 is a selectivity dopamine D-1 receptor antagonist with the Ki values of 12.6 nM and 1290 nM for dopamine D-1 receptor and dopamine D-2 receptor, respectively .
|
-
- HY-124406
-
|
|
mGluR
|
Neurological Disease
|
|
A-794282 is an antagonist with analgesic activity, selectively targeting to mGlu1 receptor that significantly reduces pain behaviors in a postoperative pain model, but motor side effects may occur at higher doses .
|
-
- HY-103360
-
|
|
CCR
|
Inflammation/Immunology
|
|
J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect .
|
-
- HY-100452
-
|
|
Orexin Receptor (OX Receptor)
|
Endocrinology
Cancer
|
|
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1 .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-100452A
-
|
OX2R antagonist
|
Orexin Receptor (OX Receptor)
|
Endocrinology
Cancer
|
|
TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1 .
|
-
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-148088
-
|
|
Adenosine Receptor
|
Cancer
|
|
M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-121383R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (Standard) is the analytical standard of Labetalol. This product is intended for research and analytical applications. Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-15691A
-
|
|
Others
|
Inflammation/Immunology
|
|
PF-4455242 hydrochloride is a selective, short-acting antagonist of the κ-opioid receptor, exhibiting potential analgesic effects. PF-4455242 hydrochloride has been identified through a strategy utilizing parallel chemistry and physicochemical property design. PF-4455242 hydrochloride demonstrated confirmed potency and selectivity in the tail-flick analgesia model.
|
-
- HY-14873
-
|
BG 9928
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure .
|
-
- HY-101764
-
|
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
|
-
- HY-121037
-
|
EGM1
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
|
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
|
-
- HY-18263A
-
|
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-18263C
-
|
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-124290
-
|
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
|
-
- HY-18263
-
|
SB-656933 hydrochloride
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-10095
-
|
BIBN-4096; BIBN 4096BS
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
|
-
- HY-15722
-
-
- HY-B0462
-
-
- HY-A0142A
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .
|
-
- HY-15067
-
DNQX
5 Publications Verification
FG 9041
|
iGluR
|
Cancer
|
|
DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
|
-
- HY-14127
-
R121919
5 Publications Verification
NBI30775
|
CRFR
|
Neurological Disease
Endocrinology
|
|
R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats .
|
-
- HY-10095A
-
|
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP .
|
-
- HY-P1473
-
|
Amylin (8-37) (mouse, rat)
|
Amylin Receptor
|
Metabolic Disease
|
|
Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
|
-
- HY-109024
-
-
- HY-10792A
-
-
- HY-19168
-
|
EAA-090
|
iGluR
|
Neurological Disease
|
|
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site .
|
-
- HY-118557
-
|
S-MPEC
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment .
|
-
- HY-108908A
-
-
- HY-P1277
-
-
- HY-103568
-
|
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders .
|
-
- HY-112596
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-112596A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-P1103
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P1167
-
-
![[Orn5]-URP](//file.medchemexpress.eu/product_pic/hy-p1167.gif)
- HY-124300
-
|
|
P2X Receptor
|
Others
|
|
JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively .
|
-
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-103547
-
|
|
GCGR
|
Metabolic Disease
|
|
L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively .
|
-
- HY-103404
-
-
- HY-107627
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
|
-
- HY-103326
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
NIDA-41020 is a potent and selective cannabinoid receptor 1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET) .
|
-
- HY-122168
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively .
|
-
- HY-107609
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BAY-u 9773 is a non-selective antagonist of the CysLT receptors (cysteinyl leukotrienes receptors) with about the same IC50 for CysLT 1 and CysLT 2. BAY-u9773 is used for the inhibition of LT responses .
|
-
- HY-108480
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity .
|
-
- HY-A0142
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Dapiprazole is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole suppresses the opioid withdrawal symptoms. Dapiprazole is also used as eye drops for reversing mydriasis .
|
-
- HY-17352
-
|
Ro 61-1790; VML 588; AXV-034343
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
|
-
- HY-105124
-
-
- HY-107730
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor .
|
-
- HY-117118A
-
-
- HY-119061
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .
|
-
- HY-14408
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .
|
-
- HY-149854A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity .
|
-
- HY-103518
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .
|
-
- HY-100961
-
|
1,3-Dipropyl-8-phenylxanthine
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
NPC 200 is a potent and selective antagonist of Adenosine A1 Receptor. NPC 200 reverses NECA-induced left and right atrial depression with EC50s of 1.08 and 2.03 μM .
|
-
- HY-115645
-
|
NBI30775 hydrochloride
|
CRFR
|
Neurological Disease
Metabolic Disease
|
|
R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats .
|
-
- HY-103518A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP36216 hydrochloride is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .
|
-
- HY-124831
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
NTRC-844 (compound 8) is a selective antagonist of neurotensin receptor type 2 (NTS2),with the EC50 of 238 nM. NTRC-844 plays an important role in analgesic animal research .
|
-
- HY-10888R
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Istradefylline (Standard) is the analytical standard of Istradefylline. This product is intended for research and analytical applications. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
|
-
- HY-117574
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
SB 207710 is a highly selective antagonist of the 5-HT4 receptor that has been shown to effectively block the positive inotropic effect induced by serotonin in human right atrial appendage preparations .
|
-
- HY-13710AR
-
|
|
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Dimethindene (maleate) (Standard) is the analytical standard of Dimethindene (maleate). This product is intended for research and analytical applications. Dimethindene maleate is a selective histamine H1 antagonist with antihistamine effects. Dimethindene maleate can be used for the research of hypersensitivity reactions .
|
-
- HY-105138
-
|
BG 9719; CVT-124
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Adentri (CVT-124) is a potent and A1-adenosine selective antagonist with a Ki of 0.45 nM at cloned human A1-receptors. Adentri can be utilized in cardiovascular research .
|
-
- HY-P2109
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
|
-
- HY-164580
-
-
- HY-N3945R
-
|
|
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Glaucine (Standard) is the analytical standard of Glaucine. This product is intended for research and analytical applications. Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 μM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities .
|
-
- HY-135976
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25?nM, 92?nM and 126?nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
|
-
- HY-10797
-
|
CJ-042794
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers .
|
-
- HY-13706
-
|
TM30089 Racemate
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2 .
|
-
- HY-P1335
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-14336
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity .
|
-
- HY-14136
-
-
- HY-18006
-
-
- HY-13206
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research .
|
-
- HY-14880B
-
|
JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .
|
-
- HY-B0411
-
|
R33812
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-10562A
-
-
- HY-14111
-
-
- HY-U00443
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
|
-
- HY-100714A
-
|
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
|
-
- HY-17000S
-
-
- HY-110230
-
|
D 9998-d4 hydrochloride
|
Potassium Channel
iGluR
|
Neurological Disease
|
|
Flupirtine-d4 (D 9998-d4) hydrochloride is the deuterium labeled Flupirtine. Flupirtine(D 9998) hydrochloride is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties .
|
-
- HY-114244
-
USL311
1 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
|
USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4 .
|
-
- HY-14880A
-
|
JNJ-31001074 dihydrochloride
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .
|
-
- HY-14880
-
|
JNJ-31001074
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .
|
-
- HY-136146
-
|
|
nAChR
|
Neurological Disease
|
|
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
|
-
- HY-13738
-
|
Keoxifene; LY156758 free base; LY139481
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-P1277A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
|
-
- HY-W011955
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor antagonist with Kis of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively .
|
-
- HY-131289
-
|
|
mGluR
|
Neurological Disease
|
|
LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression .
|
-
- HY-103233
-
|
FG 9041 disodium salt
|
iGluR
|
Cancer
|
|
DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
|
-
- HY-125989B
-
|
2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation .
|
-
- HY-14117
-
-
- HY-107616
-
|
|
LPL Receptor
Apoptosis
|
Others
|
|
H2L5186303 is an effective and selective LPA2 receptor antagonist, with an IC50 of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis .
|
-
- HY-107700
-
|
GV 150526A
|
iGluR
|
Cardiovascular Disease
|
|
Gavestinel (GV 150526A) is a potent, selective, orally active and non-competitive antagonist of NMDA receptor. Gavestinel binds to the glycine site of the NMDA receptor, with a pKi of 8.5. Gavestinel can be used for the research of acute ischemic stroke .
|
-
- HY-108481
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects .
|
-
- HY-103222
-
|
3',4'-Dimethoxy-αNF
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent .
|
-
- HY-P3881
-
-
- HY-A0033S1
-
|
UK-88525-d4
|
mAChR
|
Cancer
|
|
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
|
-
- HY-17539
-
|
|
CRM1
|
Cancer
|
|
PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE). PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1 .
|
-
- HY-107644
-
|
|
mAChR
|
Cardiovascular Disease
|
|
AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .
|
-
- HY-162231
-
|
|
Histamine Receptor
mAChR
|
Inflammation/Immunology
|
|
HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases .
|
-
- HY-14752
-
|
SB 751689
|
CaSR
|
Metabolic Disease
Endocrinology
|
|
Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis .
|
-
- HY-15104
-
|
SB 751689A
|
CaSR
|
Metabolic Disease
Endocrinology
|
|
Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret hydrochloride (SB 751689A) is used for the study of postmenopausal osteoporosis .
|
-
- HY-103418
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor
partial agonist and Dopamine D3 receptor antagonist (with pEC50 of 8.3 and <5.5 respectively) .
|
-
- HY-102092
-
|
PD 147953
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
|
-
- HY-W030796
-
|
|
Taste Receptor
Others
|
Metabolic Disease
|
|
Lactisole free acid is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit, a glucose-sensing receptor. Lactisole free acid inhibits insulin secretion induced by glucose in mouse islets .
|
-
- HY-153015
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015B
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 hydrochloride is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 hydrochloride can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015D
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 mesylate is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 mesylate can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-B0462B
-
-
- HY-103428
-
LE 300
2 Publications Verification
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay .
|
-
- HY-118198
-
|
|
Others
|
Others
|
|
NPY Y2 antagonist 1 (compound 36) is a potent, soluble pyridine analog. In summary, highly promising high-throughput screening hits were extensively explored for structure-activity relationships and a range of potency-enhancing modifications were identified. A potent, soluble, and selective NPY Y2 antagonist 36 was discovered that is amenable to in vitro screening studies. In vivo studies on this molecule will be published in due course.
|
-
- HY-167688
-
|
|
Others
|
Cardiovascular Disease
|
|
GSK-1562590 is a uropeptide-II receptor antagonist with high affinity and selectivity. GSK-1562590 exhibits significant antagonistic activity in multiple bioassays and, in contrast, displays relatively sustained receptor binding times. GSK-1562590 can inhibit human urinary peptide-II-induced aortic contraction in rats in experiments, and its effect can last for at least 24 hours .
|
-
- HY-10792
-
|
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-110186
-
|
|
Adenosine Receptor
|
Metabolic Disease
|
|
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction .
|
-
- HY-70068
-
-
- HY-10053
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
|
-
- HY-14338A
-
|
Lu AE58054 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .
|
-
- HY-13951
-
-
- HY-16346
-
-
- HY-B1196
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent .
|
-
- HY-B1238
-
|
(±)-Pronethalo
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs) .
|
-
- HY-12245
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation .
|
-
- HY-100483
-
|
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively .
|
-
- HY-19914
-
-
- HY-108539
-
CE3F4
1 Publications Verification
|
Ras
|
Cardiovascular Disease
|
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-108912
-
-
- HY-102004
-
|
SB 659032
|
Phospholipase
|
Neurological Disease
Inflammation/Immunology
|
|
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
|
-
- HY-19589
-
-
- HY-12433
-
-
- HY-13004S
-
-
- HY-114379
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia .
|
-
- HY-108707
-
|
|
iGluR
|
Neurological Disease
|
|
LY3130481 is an orally available AMPA receptor antagonist, selectively inhibiting the IC50 value of AMPA/TARP γ-8 at 65 nM. LY3130481 has anticonvulsant, antiepileptic, and pain-relieving effects .
|
-
- HY-15731
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast .
|
-
- HY-121018
-
|
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury .
|
-
- HY-14338
-
|
Lu AE58054
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .
|
-
- HY-B1238A
-
|
(±)-Pronethalo hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs) .
|
-
- HY-P1103A
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P1167A
-
-
![[Orn5]-URP TFA](//file.medchemexpress.eu/product_pic/hy-p1167a.gif)
- HY-14559
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility .
|
-
- HY-103123
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases .
|
-
- HY-119802S
-
-
- HY-N10397
-
|
|
CCR
|
Inflammation/Immunology
|
|
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases .
|
-
- HY-10888S
-
-
- HY-148232
-
|
|
CCR
|
Inflammation/Immunology
|
|
BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist (human IC50=3 nM; rat IC50=11 nM; mice IC50=81 nM) .
|
-
- HY-136935
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Alloyohimbine, an alkaloid, is a selective α2-adrenoceptor antagonist with K Dα1, K Dα2 of 0.28 μM and 0.006 μM, respectively .
|
-
- HY-103566
-
|
|
mGluR
EGFR
|
Neurological Disease
|
|
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM .
|
-
- HY-111280
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ST 198 is an orally active D3R antagonist. ST 198 can block the expression of nicotine-induced CPP at doses selective for D3R. ST 198 can be used for the research of neurological disease .
|
-
- HY-15676A
-
|
RG7388 (enantiomer)
|
Others
MDM-2/p53
|
Cancer
|
|
Idasanutlin enantiomer is the isomer of Idasanutlin (HY-15676), and can be used as an experimental control. Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
|
-
- HY-123059
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease .
|
-
- HY-107694
-
|
(Rac)-MK-801
|
Others
|
Others
|
|
(Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist .
|
-
- HY-103567
-
|
|
mGluR
|
Neurological Disease
|
|
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-13209S
-
|
BSF 208075-d10; LU 208075-d10
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
|
-
- HY-107562
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research .
|
-
- HY-14753
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder .
|
-
- HY-118238
-
|
MRZ-8456
|
mGluR
|
Neurological Disease
|
|
Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC50 of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .
|
-
- HY-103567A
-
|
|
mGluR
|
Neurological Disease
|
|
Desmethyl-YM-298198 is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-119145
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2496 is a selective P2Y1 receptor antagonist with an IC50 value of 1.5 μM, exhibiting antiplatelet aggregation activity. MRS2496 can be used in the research of antiplatelet aggregation and blood-related diseases .
|
-
- HY-106039
-
|
|
iGluR
|
Neurological Disease
|
|
LY 215490 is a selective, competitive AMPA receptor antagonist against AMPA, CGSl9755 and kainate with IC50 values of 4.8, 26.4 and 247 μM, respectively. LY 215490 shows neuroprotective effects in focal ischaemia .
|
-
- HY-107750A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .
|
-
- HY-133717
-
|
|
Opioid Receptor
TRP Channel
|
Cancer
|
|
Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer .
|
-
- HY-118557A
-
|
S-MPEC hydrochloride
|
5-HT Receptor
|
Others
|
|
Iferanserin hydrochloride (S-MPEC hydrochloride) is a selective serotonin receptor antagonist with the potential to inhibit internal hemorrhoids. Iferanserin hydrochloride demonstrated efficacy and tolerability in ongoing Phase IIb clinical trials, with the ability to significantly reduce patient-reported symptoms of bleeding and pruritus .
|
-
- HY-14940
-
|
MDL100907; M 100907
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
|
-
- HY-111925
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
|
-
- HY-120619
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively .
|
-
- HY-16489A
-
|
|
mAChR
Calcium Channel
|
Neurological Disease
|
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
|
-
- HY-107692
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit .
|
-
- HY-148088A
-
|
|
Adenosine Receptor
|
Cancer
|
|
M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-100607AR
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Landiolol (hydrochloride) (Standard) is the analytical standard of Landiolol (hydrochloride). This product is intended for research and analytical applications. Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist .
|
-
- HY-12079
-
|
|
CCR
|
Inflammation/Immunology
|
|
CP-481715 is a potent, reversible and selective CCR1 antagonist with a Kd of 9.2 nM for human CCR1. CP-481715 is >100-fold selective for CCR1 as compared with a panel of G-protein-coupled receptors including related chemokine receptors. CP-481715 has the potential for rheumatoid arthritis and other inflammatory diseases research .
|
-
- HY-B1371A
-
|
Spiroperidol hydrochloride
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
Chloride Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities .
|
-
- HY-B1517AR
-
|
(RS)-Alprenolol hydrochloride (Standard); dl-Alprenolol hydrochloride (Standard)
|
5-HT Receptor
|
Cancer
|
|
Alprenolol (hydrochloride) (Standard) is the analytical standard of Alprenolol (hydrochloride). This product is intended for research and analytical applications. Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
|
-
- HY-106874B
-
|
rel-RS-15385-197
|
Adrenergic Receptor
Prostaglandin Receptor
|
Neurological Disease
|
|
rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
|
-
- HY-110129
-
|
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-16039
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
|
-
- HY-15708
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
LY2795050 is a short-acting selective κκ-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction .
|
-
- HY-B0298A
-
|
HS-592 fumarate; Meclastine fumarate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
|
-
- HY-15319
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively .
|
-
- HY-15450A
-
|
|
CCR
|
Endocrinology
|
|
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
|
-
- HY-101946
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
|
-
- HY-103316A
-
Ned 19
2 Publications Verification
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
|
-
- HY-125839
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
|
-
- HY-11083
-
|
GW-3430
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity .
|
-
- HY-110237
-
|
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-107725
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively) .
|
-
- HY-100937
-
|
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes .
|
-
- HY-15071
-
|
|
iGluR
|
Neurological Disease
|
|
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions .
|
-
- HY-B0640A
-
|
WAL801 hydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-N7740
-
|
|
P2Y Receptor
Endogenous Metabolite
|
Others
|
|
Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors .
|
-
- HY-106277A
-
|
MEN16132
|
Bradykinin Receptor
|
Metabolic Disease
|
|
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
|
-
- HY-19668A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses [1]
|
-
- HY-100980
-
|
BE2254 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
|
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively .
|
-
- HY-19849
-
|
PGN 1531 free base
|
Prostaglandin Receptor
|
Neurological Disease
|
|
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKB of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache .
|
-
- HY-B0411A
-
|
R33812 monomaleate
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-150790
-
-
- HY-123085
-
|
Isoalloxazine
|
Adenosine Receptor
|
Cancer
|
|
Alloxazine is a selective A2b antagonist. Alloxazine completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer .
|
-
- HY-W011245
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Ranitidine S-oxide is the metabolite of Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion .
|
-
- HY-103165
-
|
|
Adenosine Receptor
|
Infection
Cancer
|
|
PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases .
|
-
- HY-15078
-
|
(R)-SPD502
|
iGluR
|
Neurological Disease
|
|
NS1219 ((R)-SPD502) is the isomer of NS 1209 HY-15074. NS1209 is a selective AMPA receptor antagonist with neuroprotective activity. NS1209 can be used for the research of stroke, neuropathic pain and epilepsy .
|
-
- HY-17610
-
|
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-106277
-
|
|
Bradykinin Receptor
|
Metabolic Disease
|
|
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
|
-
- HY-149855
-
|
|
Sigma Receptor
|
Others
|
|
AB10 is a selective S1R antagonist. AB10 with Ki of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model .
|
-
- HY-155550
-
|
|
c-Fms
|
Inflammation/Immunology
|
|
CSF1R-IN-17 (compound 9) is a potent and selective CSF1R antagonist, with an IC50 of 0.2 nM. CSF1R-IN-17 can inhibit osteoclast differentiation .
|
-
- HY-114814
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects .
|
-
- HY-17352A
-
|
Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .
|
-
- HY-106347
-
|
CR 2945
|
Cholecystokinin Receptor
|
Inflammation/Immunology
|
|
Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
|
-
- HY-120308
-
|
SR140603
|
Neurokinin Receptor
|
Neurological Disease
|
|
(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-153015A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 hydrobromide is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 hydrobromide can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015C
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 benzoate is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 benzoate can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-P5010
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R .
|
-
- HY-14552
-
|
SB 223412
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .
|
-
- HY-14552A
-
|
SB 223412 hydrochloride; SB 223412-A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .
|
-
- HY-P1335A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-110125
-
|
CID 1261822
|
GPR55
|
Neurological Disease
|
|
ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats .
|
-
- HY-123532
-
|
VUF6002
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
|
-
- HY-B0251R
-
|
Epoxymexrenone (Standard)
|
Mineralocorticoid Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Eplerenone (Standard) is the analytical standard of Eplerenone. This product is intended for research and analytical applications. Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV) .
|
-
- HY-163150
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant 5-HT6R antagonist with Ki values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease .
|
-
- HY-10088
-
|
ZD4054
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
|
-
- HY-B0640
-
|
WAL801
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-16768
-
|
QAW039; NVP-QAW039
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma .
|
-
- HY-117508
-
|
|
P2X Receptor
|
Neurological Disease
|
|
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
|
-
- HY-N2600
-
|
|
Bombesin Receptor
|
Cancer
|
|
Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
|
-
- HY-108411
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-11030
-
-
- HY-P1393
-
|
|
Amylin Receptor
|
Endocrinology
|
|
AC 187 is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .
|
-
- HY-12206
-
|
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
|
-
- HY-P1078
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
|
-
- HY-P1215
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
- HY-P1215A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
- HY-15856
-
|
cis-(Z)-Flupenthixol dihydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively .
|
-
- HY-14886
-
|
MEN16132 free base
|
Bradykinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .
|
-
- HY-12206A
-
|
MR-12842 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
|
-
- HY-N0584
-
|
6-Hydroxyhyoscyamine
|
mAChR
|
Neurological Disease
Cancer
|
|
Anisodamine (6-Hydroxyhyoscyamine), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning .
|
-
- HY-W035137
-
|
5,15-DPP
|
STAT
|
Cancer
|
|
5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist (IC50s of 0.28 µM and 10 µM for STAT3 and STAT1, respectively) .
|
-
- HY-149055
-
|
|
CXCR
|
Inflammation/Immunology
|
|
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11 .
|
-
- HY-13245B
-
|
(Rac)-INCB8761
|
CCR
|
Inflammation/Immunology
|
|
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-109171R
-
|
|
Neurokinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can be used in vasomotor and schizophrenia studies .
|
-
- HY-119802R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Practolol (Standard) is the analytical standard of Practolol. This product is intended for research and analytical applications. Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias .
|
-
- HY-119087
-
-
- HY-B0532S
-
-
- HY-109036A
-
|
(S)-RO5025181; (S)-SYN120
|
Others
|
Neurological Disease
|
|
(S)-Landipirdine ((S)-RO5025181), a selective and potent 5-HT6R antagonist, significantly impacts the hERG pharmacophore and serves as a valuable tool for investigating neurological disorders, particularly within the context of Alzheimer's disease.
|
-
- HY-B1277R
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
|
-
- HY-50674
-
|
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
- HY-10301
-
MK-3207
3 Publications Verification
|
CGRP Receptor
|
Neurological Disease
|
|
MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies .
|
-
- HY-10655
-
|
ACT-058362
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats .
|
-
- HY-B0281A
-
-
- HY-16963
-
-
- HY-17037
-
|
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-19282A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
(5R)-BW-4030W92 is the R enantiomer of BW-4030W92. BW-4030W92 is a non-selective, voltage-, and use-dependent sodium channel antagonist.
|
-
- HY-17503AS
-
-
- HY-107604
-
|
|
iGluR
|
Neurological Disease
|
|
UBP 302 is a potent and selective GLUK5-subunit containing kainate receptor antagonist (apparent Kd=402 nM), and displays very little affinity on GluK2 (GluR6) kainate receptors. Anxiolytic effects .
|
-
- HY-108682
-
-
- HY-15274
-
|
CM9; GW671021
|
Prostaglandin Receptor
|
Cancer
|
|
L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has ?micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively .
|
-
- HY-W040270
-
|
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-I0021
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-15450
-
|
|
CCR
|
Endocrinology
|
|
INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
|
-
- HY-120210
-
|
|
ROR
|
Inflammation/Immunology
Cancer
|
|
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-P1107
-
|
aSvg-30
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively .
|
-
- HY-B0693
-
-
- HY-10655A
-
|
ACT-058362 hydrochloride
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats .
|
-
- HY-118941
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure .
|
-
- HY-122219
-
|
|
CCR
|
Inflammation/Immunology
|
|
R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects .
|
-
- HY-135464
-
|
|
mGluR
|
Neurological Disease
|
|
(±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a .
|
-
- HY-102094
-
|
|
mGluR
|
Neurological Disease
|
|
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist .
|
-
- HY-108976
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively .
|
-
- HY-108234
-
|
VU 255035
|
mAChR
|
Neurological Disease
|
|
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations .
|
-
- HY-107566
-
|
|
Histamine Receptor
Parasite
|
Infection
|
|
Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3 receptor, respectively. Anti-malarial activity .
|
-
- HY-B0745S
-
-
- HY-116099
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research .
|
-
- HY-116800
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity .
|
-
- HY-101699A
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
|
-
- HY-106807
-
|
SL 81.0385
|
5-HT Receptor
|
Neurological Disease
|
|
Litoxetine (SL 81.0385) is a selective 5-HT uptake inhibitor. Litoxetine is a 5-HT3 receptor antagonist with a Ki of 85 nM for cerebral 5-HT3 receptors. Litoxetine is an antidepressant and has antiemetic properties .
|
-
- HY-12735
-
|
|
GCGR
|
Metabolic Disease
Endocrinology
|
|
SCH 900822 is a potent and selective glucagon receptor (hGCGR) antagonist that blocks the binding of glucagon to its receptor, thereby reducing hepatic glycogenolysis and gluconeogenesis, thereby lowering blood glucose production. SCH 900822 can be used in the study of type 2 diabetes .
|
-
- HY-118209
-
|
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
L-646462 is an antagonist of dopamine and 5-HT, with selectivity for the peripheral system (the central/peripheral activity ratio of L-646462 is 143). L-646462 can be used in research related to nausea, vomiting, and associated neurological disorders .
|
-
- HY-119768
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
(±)-BAK2-66 is a selectivity dopamine D3 receptor antagonist with theKi values of 1nM and 960 nM for D3R and D2R, respectively. (±)-BAK2-66 can be used for study in animal models of addiction .
|
-
- HY-111242
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SV 156 is a potent and selective D2 dopamine receptor antagonist, with a Ki of 2.5 nM for hD2. SV 156 has approximately 40-fold binding selectivity for D2 dopamine receptors compared to the D3 receptor subtype. SV 156 can be used for L-DOPA (HY-N0304)-associated abnormal involuntary movements (AIMs) research .
|
-
- HY-13243
-
|
ADL 8-2698; LY 246736
|
Opioid Receptor
|
Neurological Disease
|
|
Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
|
-
- HY-76657
-
|
ADL 8-2698 monohydrate; LY 246736 monohydrate
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .
|
-
- HY-111372
-
|
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- HY-105226
-
|
PD134308
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
|
CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .
|
-
- HY-103550
-
|
|
mGluR
|
Neurological Disease
|
|
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .
|
-
- HY-107558
-
|
VUF6002 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-105226B
-
|
PD134308 hemihydrate
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
|
CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects .
|
-
- HY-158332
-
|
SKF-95587; BM-13177
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Sulotroban (SKF-95587; BM-13177) is a selective antagonist for thromboxane A2 receptor (TXA2 Receptor). Sulotroban exhibits inhibitory activity against carbocyclic thromboxane A2- and endoperoxide-induced vasoconstrictor. Sulotroban inhibits platelets aggregation .
|
-
- HY-19692
-
|
DA 6215; U98079A
|
5-HT Receptor
|
Neurological Disease
|
|
Itasetron (DA 6215) is a selective 5-HT3 receptor antagonist. Itasetron improves spatial learning and memory abilities in the aged rat. Itasetron has potent antiemetic properties. Itasetron is used for age-related memory degeneration in rodents .
|
-
- HY-B0702
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-10799
-
|
|
Complement System
|
Cancer
|
|
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2 .
|
-
- HY-14789
-
-
- HY-A0261
-
|
ICI-50123
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
|
-
- HY-14369
-
-
- HY-P2093
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
-
- HY-108697
-
PT2399
5 Publications Verification
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo .
|
-
- HY-12308
-
|
|
Integrin
|
Inflammation/Immunology
|
|
TCS 2314 (compound 3) is orally active and selective very late antigen-4 (VLA-4, α4β1, CD49d/CD29) antagonist with an IC50 of 4.4 nM .
|
-
- HY-107734
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
Endocrinology
|
|
L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure .
|
-
- HY-129393
-
|
AB928
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities .
|
-
- HY-130248
-
|
|
GnRH Receptor
|
Endocrinology
|
|
BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels .
|
-
- HY-B2178
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-P1078A
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
|
-
- HY-P1209A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
PG106 TFA is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50= 210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor .
|
-
- HY-P2093B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
-
- HY-106408A
-
|
Salfaprodil; Neu2000 potassium
|
iGluR
|
Neurological Disease
|
|
Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death .
|
-
- HY-18200
-
|
E5555; ER-172594-00
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
|
-
- HY-124874
-
|
(rel)-Aspergillimide; (rel)-VM55598
|
nAChR
|
Neurological Disease
|
|
(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms .
|
-
- HY-12738
-
-
- HY-108657
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
|
-
- HY-103166
-
PSB-603
2 Publications Verification
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM .
|
-
- HY-130248B
-
|
|
GnRH Receptor
|
Others
|
|
(R)-BAY-899 is the R-enantiomer of BAY-899. BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively .
|
-
- HY-100834
-
|
5,7-DCKA
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures .
|
-
- HY-I0021A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus .
|
-
- HY-N11061
-
|
|
iGluR
|
Neurological Disease
|
|
Withaphysalin D is a selective antagonist against the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B. Withaphysalin D can be isolated from water lilies and has neuroprotective properties. Withaphysalin D is able to cross the blood-brain barrier .
|
-
- HY-17503S3
-
|
|
Apoptosis
Adrenergic Receptor
|
Cancer
|
|
Metoprolol-d5 is the deuterium labeled Metoprolol[1]. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[2][3][4].
|
-
- HY-101839
-
|
VU0488130
|
mAChR
|
Neurological Disease
|
|
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .
|
-
- HY-108665
-
|
FPL 66096 tetrasodium; PSFM-ATP tetrasodium
|
P2Y Receptor
|
Cardiovascular Disease
|
|
AR-C66096 tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism .
|
-
- HY-148695B
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
|
-
- HY-148695C
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
|
-
- HY-118895
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
L-641953 is an orally active, selective TXA/PG-END receptor (thromboxane-prostaglandin endoperoxide receptor) antagonist. L-641953 significantly inhibits arachidonic acid-induced bronchoconstriction. L-641953 may be used in cardiovascular disease research .
|
-
- HY-160210
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BAY-6096 is a potent, selective, and highly water-soluble adrenergic receptor α2B antagonist with an IC50 of 14 nM. BAY-6096 can effectively reduceα 2B receptor agonist-induced rat vascular contraction .
|
-
- HY-10049A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .
|
-
- HY-103115
-
|
EMD 281014; LY 2422347 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
|
-
- HY-162118
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
RGH-122 (compound 43) is an orally active, potent, selective, and hV1a receptor antagonist with Ki value of 0.3 nM and IC50 of 0.9 nM. RGH-122 showes microsomal stability with CLint value of 13/28/25 μL/min/mg .
|
-
- HY-107653
-
|
|
mAChR
|
Neurological Disease
|
|
J 104129 fumarate is a selective and orally active muscarinic M3 antagonist with Ki values of 4.2 nM and 490 nM for M3 and M2, respectively. J 104129 fumarate antagonized ACh-induced bronchoconstriction. J 104129 fumarate has the potential for the research of obstructive airway disease .
|
-
- HY-17610A
-
|
TS-091 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-16983
-
|
|
ROR
|
Inflammation/Immunology
|
|
GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-118615
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder .
|
-
- HY-17503R
-
-
- HY-19261
-
|
|
Others
|
Metabolic Disease
|
|
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
|
-
- HY-110322A
-
PPTN
2 Publications Verification
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
|
-
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-110322
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity .
|
-
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-103055
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN mesylate is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN mesylate exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
|
-
- HY-107564
-
|
VUF 4702 dihydrobromide
|
Others
|
Inflammation/Immunology
|
|
Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .
|
-
- HY-15404
-
|
Lu-135252
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
|
-
- HY-107536
-
ML 145
1 Publications Verification
|
GPR35
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM) . ML 145 has no significant activity for GPR35 at either rodent ortholog .
|
-
- HY-109118A
-
|
SUVN-502 mesylate
|
5-HT Receptor
|
Neurological Disease
|
|
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
|
-
- HY-100971
-
|
AMI-193
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity .
|
-
- HY-14940A
-
|
(S)-MDL100907; (S)-M 100907
|
5-HT Receptor
|
Neurological Disease
|
|
(S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
|
-
- HY-105093
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
N-0861 is a novel selective A1 adenosine receptor antagonist. In studies, it has been shown to be able to inhibit the negative conduction effects (prolonged AH interval) and chest pain caused by adenosine, while having no significant effect on the increase in coronary blood flow velocity caused by adenosine. This indicates that N-0861 has the property of selectively inhibiting A1 adenosine receptors .
|
-
- HY-19532S
-
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-A0015
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-13459
-
|
|
Smo
|
Cancer
|
|
PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
|
-
- HY-B0192A
-
|
SL 77499-10
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-B0192
-
|
SL 77499
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-B0233
-
|
PN 200-110
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-14450
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-31020028 is a selective and brain penetrant antagonist of neuropeptide Y Y2 receptor with pIC50 values of 8.07 and 8.22 for human and rat Y2 receptor, respectively. JNJ-31020028 can be used for the research of nervous disease .
|
-
- HY-15043
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
|
-
- HY-100371
-
|
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons .
|
-
- HY-14751
-
|
SCH619734
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-108677
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .
|
-
- HY-123820
-
|
|
mGluR
|
Neurological Disease
|
|
LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM . LY3020371 hydrochloride exerts an antidepressant-like signature in vivo .
|
-
- HY-112693
-
|
|
STING
|
Inflammation/Immunology
|
|
H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .
|
-
- HY-14263
-
|
Propericiazine; RP 8909
|
Dopamine Receptor
|
Neurological Disease
|
|
Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis . Pericyazine is a selective D2-dopamine receptor antagonist . Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects .
|
-
- HY-101483
-
|
|
Others
|
Neurological Disease
Cancer
|
|
Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs .
|
-
- HY-P2093A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
-
- HY-15084B
-
|
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
|
-
- HY-120568
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
M4284 is a selective and orally active biphenyl mannoside FimH antagonist. M4284 has activities against different UPEC (Urinary tract infections (UTI) caused by uropathogenic E. coli) strains in different host genetic backgrounds and gut microbial community contexts .
|
-
- HY-130411
-
|
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-P1393A
-
|
|
Amylin Receptor
|
Endocrinology
|
|
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-P1209
-
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
-
- HY-103551A
-
|
|
mGluR
|
Neurological Disease
|
|
LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively .
|
-
- HY-109176
-
|
GDC-9545; RG6171
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
|
-
- HY-13459A
-
|
|
Smo
|
Cancer
|
|
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
|
-
- HY-15319A
-
|
|
CXCR
|
Cancer
|
|
(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively .
|
-
- HY-138161
-
JR14a
2 Publications Verification
|
Complement System
|
Inflammation/Immunology
|
|
JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation .
|
-
- HY-117575A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties .
|
-
- HY-17503BS
-
-
- HY-12182
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-P0039
-
|
|
Bombesin Receptor
|
Cancer
|
|
BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer .
|
-
- HY-15546
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .
|
-
- HY-107605
-
|
|
iGluR
|
Neurological Disease
|
|
UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices .
|
-
- HY-110036
-
-
- HY-103454B
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
|
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-145425
-
|
|
IRE1
|
Cancer
|
|
PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing .
|
-
- HY-W062109
-
|
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
|
-
- HY-14751A
-
|
SCH619734 hydrochloride
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-17037A
-
|
LS 519 free base; Pirenzepin; Gastrozepin
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-16436
-
|
SCH619734 hydrochloride hydrate
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-113936
-
-
- HY-152170
-
|
|
nAChR
|
Neurological Disease
|
|
bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
|
-
- HY-160440
-
|
|
Others
|
Others
|
|
rel-VU6021625 is the less active relative configuration of VU6021625 (HY-160440A). VU6021625 is a potent and selective mAChR M4 antagonist with IC50 values of 0.44 nM and 57 nM for human M4, rat M4, respectively .
|
-
- HY-90010R
-
|
Kabi-2234 (Standard); PNU-200583E (Standard)
|
mAChR
|
Neurological Disease
|
|
Tolterodine (tartrate) (Standard) is the analytical standard of Tolterodine (tartrate). This product is intended for research and analytical applications. Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-10562R
-
|
|
5-HT Receptor
Potassium Channel
Autophagy
|
Neurological Disease
|
|
Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
|
-
- HY-12717R
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Phentolamine (Standard) is the analytical standard of Phentolamine. This product is intended for research and analytical applications. Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-118768
-
|
|
Others
|
Neurological Disease
|
|
FMS586 free base is a selective neuropeptide Y Y5 receptor antagonist with oral activity. FMS586 can completely block the significant increase in adrenocorticotropic hormone (ACTH) and cortisol caused by the Y(5) selective agonist hPP. FMS586 also reversed the significant upregulation of adrenocorticotropic hormone (CRF) and antidiuretic hormone (AVP) mRNA expression induced by central injection of hPP. FMS586 provides the first evidence that selective stimulation of Y(5) receptors triggers activation of the HPA axis .
|
-
- HY-19409
-
|
|
Calcium Channel
|
Neurological Disease
|
|
AJG049 is a novel antagonist of the Ca 2+ channel with an IC50 value of 79 nM. AJG049 can be used to reduce the contraction of intestinal smooth muscle .
|
-
- HY-76657A
-
|
ADL 8-2698 dihydrate; LY 246736 dihydrate
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
|
-
- HY-111767
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor .
|
-
- HY-13457
-
TCN 201
1 Publications Verification
|
iGluR
|
Neurological Disease
|
|
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) .
|
-
- HY-103457
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
|
-
- HY-108554
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
|
-
- HY-116623
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
A-123189 is a selective and potent α1D antagonist with Kis of 0.312 and 0.17 for human α1D and rat α1D, respectively. A-123189 displays selectivities between 10- to 20-fold for the α1D receptor over the human α1A and rat α1A receptors .
|
-
- HY-109743
-
|
|
Others
|
Neurological Disease
|
|
BP14979 is a dopamine D3 receptor agonist with activity in the study of neurological diseases. BP14979 can be used to develop ligands with higher selectivity and affinity for D3 receptors. The structural characteristics of BP14979 make it potential in modulating the efficacy of D3 receptors. The design of BP14979 is based on the difference in efficacy with D3R selective antagonists, providing opportunities for optimizing new drug development .
|
-
- HY-W184837
-
|
KR-1008
|
Calcium Channel
|
Cardiovascular Disease
|
|
m-Nisoldipine (KR-1008) is a dihydropyridine calcium antagonist that can significantly increase cardiac output and heart index, significantly reduce the negative inotropic effect on the myocardium, and has a relatively high selectivity for the thoracic aorta. m-Nisoldipine can be used in the research of cardiovascular diseases .
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13993
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD) .
|
-
- HY-B0309
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier .
|
-
- HY-15996
-
|
VT-464
|
Cytochrome P450
Androgen Receptor
|
Cancer
|
|
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
|
-
- HY-106408
-
|
Salfaprodil free base; Neu2000
|
iGluR
|
Neurological Disease
|
|
Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death .
|
-
- HY-19837
-
|
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
|
-
- HY-B0411S
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
|
-
- HY-11030A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor .
|
-
- HY-107515
-
|
|
mGluR
|
Neurological Disease
|
|
LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects .
|
-
- HY-101232
-
|
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
|
-
- HY-120738
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects .
|
-
- HY-135903
-
|
GDC-9545 tartrate; RG6171 tartrate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
|
-
- HY-14335
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors .
|
-
- HY-W011040
-
-
- HY-11028
-
|
PF-2413873
|
Progesterone Receptor
|
Endocrinology
|
|
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo .
|
-
- HY-107515A
-
|
|
mGluR
|
Neurological Disease
|
|
LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects .
|
-
- HY-P1107A
-
|
aSvg-30 TFA
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively .
|
-
- HY-100970
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM) .
|
-
- HY-14250A
-
|
|
Androgen Receptor
|
Endocrinology
|
|
(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia .
|
-
- HY-14136S
-
-
- HY-108624
-
-
- HY-A0261A
-
|
ICI-50123 meglumine
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
|
-
- HY-108657A
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
|
-
- HY-148514
-
|
|
PDGFR
|
Cancer
|
|
CT52923 is a selective, orally active platelet-derived growth factor receptor (PDGFR) antagonist. CT52923 also is an ATP-competitive inhibitor. CT52923 can be used for the research variety of pathological diseases, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer .
|
-
- HY-132222
-
|
|
TRP Channel
|
Cancer
|
|
SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases .
|
-
- HY-B0321S
-
|
Ro 1-7683-d3
|
mAChR
|
Neurological Disease
|
|
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
|
-
- HY-108678
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Neurological Disease
|
|
TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models .
|
-
- HY-13993B
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD) .
|
-
- HY-108633
-
|
|
PARP
|
Cancer
|
|
AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism .
|
-
- HY-162284
-
|
|
ADAMTS
|
Cardiovascular Disease
|
|
BAY-9835 is a potent and orally active ADAMTS7 and ADAMTS12 antagonist with IC50s of 6 nM and 30 nM, respectively. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the atherogenesis research .
|
-
- HY-13955R
-
|
BIBR 277 (Standard)
|
Angiotensin Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
|
|
Telmisartan (Standard) is the analytical standard of Telmisartan. This product is intended for research and analytical applications. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
|
-
- HY-B0321R
-
|
Ro 1-7683 (Standard)
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Standard) is the analytical standard of Tropicamide. This product is intended for research and analytical applications. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
|
-
- HY-145480
-
|
Silodosin β-D-glucuronide sodium
|
Drug Metabolite
|
Others
|
|
Silodosin Glucuronide sodium (Silodosin β-D-glucuronide sodium) is the metabolite of Silodosin (HY-10122). Silodosin is a selective and orally active antagonist for α1A-adrenergic receptor (α1A-AR) with Ki of 0.036 nM .
|
-
- HY-129333
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Metabolic Disease
|
|
L-364918 is a potent and selective oxytocin and arginine vasopressin antagonist with Ki values of 30, 1300, 2400 nM for OT, AVP-V1, AVP-V2, respectively. L-364918 has the potential for the research of preterm labor and disturbances in water balance .
|
-
- HY-120239
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 63-0563 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values ??of 7.83 and 7.91 for rat and human 5-HT6 receptors, respectively. Ro 63-0563 has no affinity for other receptors .
|
-
- HY-14335A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 dihydrochloride is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 dihydrochloride has no affinity at other receptors .
|
-
- HY-10349
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist .
|
-
- HY-117063
-
|
|
Others
|
Endocrinology
|
|
LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity .
|
-
- HY-14567
-
|
FUB-359
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-15289
-
|
FUB 359 maleate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-B0002A
-
|
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery .
|
-
- HY-13993A
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD) .
|
-
- HY-15834A
-
|
SKF-108566J
|
Angiotensin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-B0567
-
|
|
Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
|
Infection
Cancer
|
|
Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
|
-
- HY-15894A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM .
|
-
- HY-B1396
-
|
BMY-13754; MJ-13754-1
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
|
-
- HY-109593
-
-
- HY-13213
-
|
AM211 free acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
|
-
- HY-13738S
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
|
-
- HY-13955S1
-
-
- HY-13955S
-
-
- HY-112710
-
|
|
Glucocorticoid Receptor
|
Endocrinology
Cancer
|
|
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity. ORIC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13738S2
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d4 (hydrochloride) is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
|
-
- HY-13738S3
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
|
-
- HY-125292
-
|
|
Histone Methyltransferase
Ligands for E3 Ligase
|
Cancer
|
|
NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity .
|
-
- HY-108559
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
|
-
- HY-100672
-
-
- HY-103200
-
-
- HY-103454
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
|
MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-19435A
-
|
|
iGluR
Cytochrome P450
|
Neurological Disease
|
|
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1 .
|
-
- HY-116042
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .
|
-
- HY-101043
-
|
|
Sigma Receptor
iGluR
|
Neurological Disease
|
|
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
|
-
- HY-103190
-
|
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
|
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system . MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo .
|
-
- HY-18200B
-
|
E5555 hydrobromide; ER 172594-06
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease .
|
-
- HY-107726A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIBP3226 is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 displays anxiogenic-like effect .
|
-
- HY-108563
-
|
|
Prostaglandin Receptor
|
Neurological Disease
|
|
SC 51089 is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 exhibits neuroprotective activity .
|
-
- HY-B0462AS
-
-
- HY-108683
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders .
|
-
- HY-D1199
-
|
|
P2X Receptor
P2Y Receptor
|
Inflammation/Immunology
|
|
Blue FPG-A trisodium is a selective antagonist of P2X1 receptor and P2Y1 receptor with IC50 values of 35.5 μM and 2.6 μM, respectively. Blue FPG-A trisodium is a structural isomer of the components of Reactive Blue 2 (RB2) .
|
-
- HY-108670
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM .
|
-
- HY-107562A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ-10181457 is a selective non-imidazole histamine H3 receptor antagonist that normalizes acetylcholine neurotransmission . JNJ-10181457 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-101230
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom .
|
-
- HY-157220
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation .
|
-
- HY-110036A
-
|
L768242 hydrochloride
|
Cannabinoid Receptor
|
Neurological Disease
|
|
GW-405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 hydrochloride also behaves as a noncompetitive CB1 antagonist. GW-405833 hydrochloride suppresses inflammatory and neuropathic pain .
|
-
- HY-13738AR
-
|
Keoxifene (hydrochloride)(Standard); LY156758(Standard); LY139481 hydrochloride (Standard)
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
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-
- HY-14137R
-
|
|
Cannabinoid Receptor
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Rimonabant (Hydrochloride) (Standard) is the analytical standard of Rimonabant (Hydrochloride). This product is intended for research and analytical applications. Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
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-
- HY-B0140R
-
|
|
Phosphodiesterase (PDE)
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
Aminophylline (Standard) is the analytical standard of Aminophylline. This product is intended for research and analytical applications. Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research .
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-
- HY-107626
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities .
|
-
- HY-19435
-
|
|
iGluR
Cytochrome P450
|
Neurological Disease
|
|
GYKI-47261 is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 is also a potent inducer of CYP2E1 .
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-
- HY-14567A
-
|
FUB-359 hydrochloride
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan hydrochloride displays low apparent affinity at other receptor subtypes. Ciproxifan hydrochloride can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-N0584AR
-
|
|
mAChR
|
Inflammation/Immunology
|
|
Anisodamine (hydrobromide) (Standard) is the analytical standard of Anisodamine (hydrobromide). This product is intended for research and analytical applications. Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
|
-
- HY-116958
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active .
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-
- HY-11085
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
T-226296 is an oral active and selective melanin-concentrating hormone receptor antagonist with the IC50 values of 5.5 nM and 8.6 nM for human SLC-1 and rat SLC-1, respectively. T-226296 can be used for study of obesity and insulin resistance .
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-
- HY-123676
-
|
PNU-101387G mesylate; U-101387G mesylate
|
Dopamine Receptor
|
Neurological Disease
|
|
Sonepiprazole mesylate is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-13213A
-
-
- HY-101699
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
AMG-076 free base is an orally bioavailable and selective MCHR1 antagonist. AMG-076 free base results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
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-
- HY-121053A
-
|
WY-50324 hydrochloride; SEB-324 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Adatanserin hydrochloride is a high affinity, selective and partial agonist for the 5-HT1A receptor with a Ki of 1 nM. Adatanserin hydrochloride is a moderate affinity 5-HT2 receptor antagonist with a Ki of 73 nM. Adatanserin hydrochloride shows significant anxiolytic and antidepressant activity in an animal conflict model .
|
-
- HY-116216
-
|
|
Bombesin Receptor
|
Cancer
|
|
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM . PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist . PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively .
|
-
- HY-108662
-
|
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
Cancer
|
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma .
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-
- HY-129296
-
|
|
Others
|
Neurological Disease
|
|
YM-44781 free acid is a non-peptide neuropeptide receptor antagonist with efficient NK(2) and NK(1) receptor antagonist activity. YM-44781 exhibits significant binding affinity on the NK(2) receptor (pKi = 9.94) and also on the NK(1) receptor Higher binding affinity (pKi = 9.09). In addition, YM-44781 also showed significant inhibitory effects on bladder contraction induced by selective NK(1) receptor agonists .
|
-
- HY-106874
-
|
RS-15385-197
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
|
-
- HY-14336A
-
|
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM) .
|
-
- HY-14940S
-
|
MDL100907-d4 hydrochloride; M 100907-d4 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].
|
-
- HY-100609
-
|
|
Melatonin Receptor
|
Neurological Disease
|
|
4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity) .
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-
- HY-120295
-
|
|
Endothelin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
|
-
- HY-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-122171
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
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-
- HY-106874A
-
|
RS-15385-197 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
|
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-10046
-
|
AMD 3100; JM3100; SID791
|
CXCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
|
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
|
-
- HY-17000
-
|
OPC-41061
|
Vasopressin Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia .
|
-
- HY-100832
-
UNC3866
2 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
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-
- HY-14137S
-
|
|
Isotope-Labeled Compounds
Cannabinoid Receptor
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
|
-
- HY-103234A
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
|
-
- HY-14858
-
|
SLV 320
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats .
|
-
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-P3057
-
-
![[D-Trp11]-Neurotensin](//file.medchemexpress.eu/product_pic/hy-p3057.gif)
- HY-103111
-
|
|
mGluR
|
Neurological Disease
|
|
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
|
-
- HY-107503
-
|
|
mGluR
|
Neurological Disease
|
|
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
|
-
- HY-141487
-
-
- HY-108673
-
|
|
P2X Receptor
|
Cancer
|
|
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM) .
|
-
- HY-14794
-
|
(1R,2S)-milnacipran; F2696
|
Serotonin Transporter
|
Metabolic Disease
|
|
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-15731S
-
-
- HY-101484A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
NE-100 (hydrochloride) is a potent and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 (hydrochloride) exerts antipsychotic activity in vivo[1]. NE-100 (hydrochloride) also suppresses ER stress-induced hippocampal cell death[2].
|
-
- HY-103175
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia .
|
-
- HY-13955S2
-
-
- HY-B1196A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride, an atypical neuroleptic agent, is a selective dopamine D2-receptor antagonist with little propensity for causing catalepsy and sedation. The IC50 values of Tiapride are 1440, 45.8, >100, and 11.7 μM for D1; D2; D3; D4, respectively .
|
-
- HY-103234
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
|
-
- HY-135507
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions .
|
-
- HY-12182A
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-100783B
-
|
(+)-Bicuculline methobromide; d-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders .
|
-
- HY-100413
-
|
|
Proton Pump
|
Inflammation/Immunology
|
|
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. CS-526 inhibits H +,K +-ATPase activity. CS-526 inhibits gastric acid secretion and prevents esophageal lesions. CS-526 has the potential for the research of gastroesophageal reflux disease .
|
-
- HY-103234B
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
|
-
- HY-13245A
-
|
(s)-INCB8761
|
Others
|
Inflammation/Immunology
Endocrinology
|
|
(s)-PF-4136309 is the isomer of PF-4136309 (HY-13245), and can be used as an experimental control. PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-105896
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties .
|
-
- HY-109042
-
|
CORT 125134
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
|
-
- HY-B0462R
-
|
|
Histamine Receptor
SARS-CoV
|
Infection
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Azelastine (hydrochloride) (Standard) is the analytical standard of Azelastine (hydrochloride). This product is intended for research and analytical applications. Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine hydrochloride can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
|
-
- HY-14794A
-
|
(1S,2R)-Milnacipran; F2695
|
Serotonin Transporter
|
Metabolic Disease
|
|
Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-P10427
-
|
|
CXCR
HIV
|
Infection
|
|
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-19665
-
|
LY303870
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .
|
-
- HY-117862
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guinea pig bronchial asthma models .
|
-
- HY-131821
-
|
Thymidine-5'-O-monophosphorothioate
|
P2Y Receptor
|
Others
|
|
5'-TMPS (Thymidine-5'-O-monophosphorothioate) is a selective partial agonist of P2Y6R and an antagonist of P2Y14R. Additionally, 5'-TMPS acts as a positive regulator of angiogenesis, exhibiting pro-angiogenic effects
|
-
- HY-17503AR
-
|
|
Adrenergic Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Metoprolol (succinate) (Standard) is the analytical standard of Metoprolol (succinate). This product is intended for research and analytical applications. Metoprolol succinate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol succinate shows anti-inflammation, antitumor and anti-angiogenic properties .
|
-
- HY-17503BR
-
|
|
Adrenergic Receptor
Apoptosis
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Metoprolol (tartrate) (Standard) is the analytical standard of Metoprolol (tartrate). This product is intended for research and analytical applications. Metoprolol tartrate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol tartrate shows anti-inflammation, antitumor and anti-angiogenic properties .
|
-
- HY-18346
-
|
OPC-31260
|
Vasopressin Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-114263
-
NXT629
3 Publications Verification
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
|
-
- HY-103112
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
- HY-103152
-
-
- HY-121119
-
|
|
Adenosine Receptor
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .
|
-
- HY-103112A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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-
- HY-123593
-
|
OPC-31260 hydrochloride
|
Vasopressin Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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-
- HY-107732
-
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|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
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-
- HY-103112B
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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-
- HY-107436
-
LE135
1 Publications Verification
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RAR/RXR
TRP Channel
|
Neurological Disease
Cancer
|
|
LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5?μM and 20?μM, respectively .
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-
- HY-12697A
-
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|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .
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-
- HY-107479
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
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-
- HY-109118
-
|
SUVN-502 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
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-
- HY-12697
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
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-
- HY-103177
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice .
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-
- HY-107628
-
|
|
Melatonin Receptor
|
Neurological Disease
|
|
N-Pentanoyl 2-benzyltryptamine is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. N-Pentanoyl 2-benzyltryptamine shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. N-Pentanoyl 2-benzyltryptamine can inhibit melatonin-induced enhancement of electrically-evoked responses .
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-
- HY-111385
-
|
|
Dopamine Receptor
5-HT Receptor
Arrestin
|
Neurological Disease
|
|
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
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-
- HY-117213
-
|
S1P1-IN-Ex26
|
LPL Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach .
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- HY-111372S
-
|
BAY 94-8862-d3
|
Mineralocorticoid Receptor
|
Others
|
|
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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-
- HY-111372R
-
|
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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-
- HY-159802
-
|
|
Others
|
Endocrinology
|
|
Tolamolol is a selective beta-adrenergic antagonist with significant activity in reducing exercise-induced ST-segment depression. Tolamolol is clinically equivalent to propranolol in suppressing angina and exhibits greater cardiac selectivity. Tolamolol is effective in reducing the frequency of angina attacks and the amount of glyceryl trinitrate used. Tolamolol is effective in lowering blood pressure and has a positive effect on increasing the amount of exercise that can be performed before angina attacks. The use of Tolamolol also helps improve the suppression of arrhythmias .
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-
- HY-19097
-
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Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action. Ro-24-4736 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-101641
-
-
- HY-16635
-
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ACT-129968; KYTH-105
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis .
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-
- HY-10119
-
|
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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-
- HY-B0539S
-
-
- HY-B0725S
-
|
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
|
|
Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
|
-
- HY-B0539S1
-
-
- HY-131349
-
|
|
CCR
|
Cancer
|
|
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity .
|
-
- HY-125176
-
G907
1 Publications Verification
|
Bacterial
|
Infection
|
|
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
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-
- HY-130249
-
|
|
GnRH Receptor
|
Endocrinology
|
|
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels .
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-
- HY-108625
-
SHA 68
1 Publications Verification
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Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
|
-
- HY-109012A
-
|
JNJ-42847922 hydrochloride
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
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-
- HY-107726
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIBP3226 TFA is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 TFA displays anxiogenic-like effect .
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-
- HY-100912
-
|
|
Phosphodiesterase (PDE)
Myosin
Apoptosis
Calmodulin
|
Cancer
|
|
W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 μM, respectively . W-7 hydrochloride induces apoptosis and has antitumor activity .
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-
- HY-136281
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics .
|
-
- HY-107701
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity .
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-
- HY-U00302
-
|
|
mAChR
|
Inflammation/Immunology
|
|
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
|
-
- HY-117743
-
|
SKF-108566J free base
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-131349A
-
|
|
CCR
|
Metabolic Disease
Cancer
|
|
CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity .
|
-
- HY-103530
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .
|
-
- HY-107652
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-110146
-
|
|
mGluR
|
Neurological Disease
|
|
XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms .
|
-
- HY-137976
-
|
Penequinine hydrochloride
|
mAChR
NF-κB
|
Inflammation/Immunology
|
|
Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
|
-
- HY-B0539S3
-
-
- HY-142119
-
|
|
mAChR
NF-κB
|
Inflammation/Immunology
|
|
Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
|
-
- HY-106840A
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
|
-
- HY-118497
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-149337
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
|
-
- HY-103146
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction .
|
-
- HY-P1108
-
|
|
CFTR
|
Others
|
|
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-19881
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has Ki values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research. .
|
-
- HY-13738R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Standard) is the analytical standard of Raloxifene. This product is intended for research and analytical applications. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-B0411R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (Standard) is the analytical standard of Domperidone. This product is intended for research and analytical applications. Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
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-
- HY-100832A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
|
-
- HY-W650803
-
|
A-57219
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nemazoline (A-57219) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
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-
- HY-108055
-
|
|
Urotensin Receptor
Others
|
Cardiovascular Disease
|
|
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
|
-
- HY-B0305A
-
|
HOE 760
|
Histamine Receptor
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity .
|
-
- HY-16935
-
|
JNJ-39439335
|
TRP Channel
|
Neurological Disease
|
|
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
|
-
- HY-12378
-
BQ-123
2 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-B1330
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .
|
-
- HY-15010
-
-
- HY-10791
-
-
- HY-N6776
-
|
|
Potassium Channel
|
Neurological Disease
Cancer
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
|
-
- HY-50688
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
|
-
- HY-107623
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R . TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively .
|
-
- HY-103354
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .
|
-
- HY-133017
-
|
SAR439859
|
Estrogen Receptor/ERR
|
Cancer
|
|
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER + breast cancer.
|
-
- HY-108425B
-
|
(Rac)-AMG8380
|
Sodium Channel
|
Neurological Disease
|
|
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
|
-
- HY-10119A
-
|
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-137451
-
|
S-600918
|
P2X Receptor
|
Neurological Disease
|
|
Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect .
|
-
- HY-B0251S
-
|
Epoxymexrenone-d3
|
Mineralocorticoid Receptor
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
|
-
- HY-110098
-
|
EPPTB
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
|
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids .
|
-
- HY-116020
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease .
|
-
- HY-108659
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research .
|
-
- HY-B0305
-
|
|
Histamine Receptor
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity .
|
-
- HY-151546
-
|
|
P2X Receptor
|
Neurological Disease
|
|
MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
|
-
- HY-13738S4
-
|
Keoxifene-d10; LY156758(free base)-d10; LY139481-d10
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
|
-
- HY-123206
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea .
|
-
- HY-N10132
-
|
|
nAChR
|
Infection
Neurological Disease
|
|
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
|
-
- HY-113758
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4 .
|
-
- HY-14466
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain .
|
-
- HY-16346R
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect .
|
-
- HY-121053
-
|
WY-50324; SEB-324
|
5-HT Receptor
|
Neurological Disease
|
|
Adatanserin (WY-50324) is a high affinity, selective and partial agonist for the 5-HT1A receptor with a Ki of 1 nM. Adatanserin is a moderate affinity 5-HT2 receptor antagonist with a Ki of 73 nM. Adatanserin shows significant anxiolytic and antidepressant activity in an animal conflict model .
|
-
- HY-161873
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN) .
|
-
- HY-120820
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
|
-
- HY-B1196R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride (hydrochloride) (Standard) is the analytical standard of Tiapride (hydrochloride). This product is intended for research and analytical applications. Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent .
|
-
- HY-120878
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM .
|
-
- HY-116163
-
|
CYM50202
|
Others
|
Others
|
|
ML350 (CYM50202) is a highly potent OPRK1 antagonist with selectivity and broad biological applications. With IC50 values of 9-16 nM, ML350 shows high selectivity for OPRK1, with selectivity of 219-382-fold and 20-35-fold relative to OPRD1 and OPRM1, respectively. ML350 exhibited favorable characteristics in in vivo pharmacokinetic analysis, including high passive membrane permeability and moderate human plasma protein binding. Extensive screening of ML350 against multiple ion channels, receptors, and transporters showed that it does not have adverse off-target effects .
|
-
- HY-112741
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca 2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity .
|
-
- HY-101061
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research .
|
-
- HY-13104
-
|
|
P2Y Receptor
Apoptosis
|
Cardiovascular Disease
|
|
MRS 2578 is a selective and potent P2Y6 receptor antagonist with IC50s of 37 nM (human) and 98 nM (rat). MRS 2578 exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors .
|
-
- HY-14914
-
-
- HY-15703
-
QNZ46
1 Publications Verification
|
iGluR
|
Neurological Disease
|
|
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).
|
-
- HY-A0030
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-13315S1
-
|
MK0476-d6
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
|
-
- HY-13315S
-
|
MK0476-d6 free acid
|
Isotope-Labeled Compounds
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
|
-
- HY-P1202
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively .
|
-
- HY-P1202A
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively .
|
-
- HY-108669
-
|
|
P2X Receptor
|
Neurological Disease
Cancer
|
|
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth .
|
-
- HY-11044
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
|
-
- HY-103355
-
YM022
2 Publications Verification
|
CCR
|
Metabolic Disease
|
|
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
|
-
- HY-70053
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-16952A
-
|
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders .
|
-
- HY-P1216A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
|
-
- HY-P1263
-
-
- HY-14328
-
|
PNU-101387G; U-101387G
|
Dopamine Receptor
|
Neurological Disease
|
|
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-P1264
-
|
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
|
-
- HY-18663B
-
|
|
iGluR
|
Neurological Disease
|
|
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-50674A
-
|
|
CCR
|
Inflammation/Immunology
|
|
INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity .
|
-
- HY-134189
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
|
-
- HY-12378A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-14250
-
|
|
Androgen Receptor
|
Endocrinology
|
|
PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .
|
-
- HY-103407A
-
|
|
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
PD 168568 dihydrochloride is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 dihydrochloride contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 dihydrochloride can be used for glioblastoma (GBM) research .
|
-
- HY-108658
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity .
|
-
- HY-P1102
-
TC14012
2 Publications Verification
|
CXCR
HIV
|
Infection
Cancer
|
|
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
|
-
- HY-10835
-
DG-041
2 Publications Verification
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier .
|
-
- HY-101911
-
5-BDBD
2 Publications Verification
|
P2X Receptor
|
Neurological Disease
|
|
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG) .
|
-
- HY-108509
-
|
BMY-14802-1; BMS 181100 hydrochloride
|
Sigma Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .
|
-
- HY-18166
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ 35S assays .
|
-
- HY-145086
-
|
|
Others
|
Metabolic Disease
|
|
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
|
-
- HY-108626
-
|
NCGC84
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
|
-
- HY-103224
-
|
|
PI3K
|
Cancer
|
|
PIT-1 is a selective PIP3 (phosphatidylinositol 3,4,5-trisphosphate) antagonist. PIT-1 inhibits cancer cell survival and induces apoptosis by inhibition of PIP3 dependent PI3K / Akt signaling. PIT-1 exhibits antitumor activity in vivo .
|
-
- HY-50848
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP) .
|
-
- HY-103327
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-18663A
-
|
|
iGluR
|
Neurological Disease
|
|
CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-105215
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
|
-
- HY-110198
-
|
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
|
-
- HY-147707
-
|
|
Cannabinoid Receptor
|
Others
|
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
|
-
- HY-B1794
-
-
- HY-137790
-
|
(+)-Bicuculline methochloride; d-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders .
|
-
- HY-101172
-
|
EP-A-501322
|
5-HT Receptor
|
Cardiovascular Disease
|
|
RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .
|
-
- HY-108563A
-
|
|
Prostaglandin Receptor
|
Neurological Disease
|
|
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity .
|
-
- HY-103407
-
|
|
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research .
|
-
- HY-18663
-
|
|
iGluR
|
Neurological Disease
|
|
CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-127133
-
|
MPP
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-13955S3
-
|
BIBR 277-d7
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
|
-
- HY-103375
-
|
|
CRFR
|
Neurological Disease
|
|
SN003 is a reversible antagonist of corticotropin releasing factor receptor 1 (CRFR 1) (IC50 = 241 nM) that displays more than 1000-fold selectivity over CRFR 2. SN003 suppresses CRF-induced ACTH release in vitro. SN003 attenuates depressive-like behavior in rat .
|
-
- HY-121764
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
MPCI is a cell-permeant MC4R-selective ligand with pharmacological chaperone activity. MPCI is a MC4R antagonist with a Ki value of 0.218 μM on HEK293 cells expressing hMC4R. MPCI can be used for the research of MC4R-deficient obesity .
|
-
- HY-124223
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-100834A
-
|
5,7-DCKA sodium
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (sodium) is the sodium form of 5,7-Dichlorokynurenic acid (HY-100834). 5,7-Dichlorokynurenic acid is a selective and competitive antagonist of the glycine site on the NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduces NMDA-induced neuron injury in rat cortical cell cultures .
|
-
- HY-P1108A
-
|
|
CFTR
|
Others
|
|
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-B0539R
-
-
- HY-125314
-
|
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells .
|
-
- HY-B0298AR
-
|
HS-592 fumarate (Standard); Meclastine fumarate (Standard)
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Clemastine (fumarate) (Standard) is the analytical standard of Clemastine (fumarate). This product is intended for research and analytical applications. Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
|
-
- HY-B0640AR
-
|
WAL801 hydrochloride (Standard)
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Epinastine (hydrochloride) (Standard) is the analytical standard of Epinastine (hydrochloride). This product is intended for research and analytical applications. Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-108411R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine (Standard) is the analytical standard of Emedastine. This product is intended for research and analytical applications. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-107701A
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 78608 is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). CGP 78608 has anticonvulsant activities .
|
-
- HY-123663
-
|
PNU-101958 maleate
|
Dopamine Receptor
|
Neurological Disease
|
|
U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC50 of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic .
|
-
- HY-14128
-
|
SB-723620
|
CRFR
|
Neurological Disease
|
|
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.
|
-
- HY-119097
-
|
|
mGluR
|
Neurological Disease
|
|
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .
|
-
- HY-107566A
-
|
|
Histamine Receptor
Parasite
|
Infection
|
|
Conessine dihydrobromide is a steroidal alkaloid and an effective, selective histamine H3 receptor antagonist with Ki values of 5.4, 6.0, 5.7, and 25 nM for human, dog, guinea pig, and rat H3 receptors, respectively. Conessine dihydrobromide exhibits antimalarial activity and can be used in infection-related research .
|
-
- HY-15086
-
|
CGS 19755
|
iGluR
|
Neurological Disease
|
|
Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM .
|
-
- HY-14328A
-
|
PNU-101387G hydrochloride; U-101387G hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Sonepiprazole (PNU-101387G) hydrochloride is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-100815
-
|
|
iGluR
|
Neurological Disease
|
|
(R)-AMPA is an inactive AMPA receptor ligand that inhibits the release of excitatory amino acids from neurons. (R)-AMPA is inactive in experiments that enhance the release of [3H]D-aspartate induced by electrical stimulation. (R)-AMPA is inhibited by competitive and noncompetitive AMPA receptor selective antagonists in response to AMPA and glutamate .
|
-
- HY-12193
-
|
|
Histamine Receptor
|
Others
|
|
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
|
-
- HY-15257
-
|
AFQ056
|
mGluR
|
Neurological Disease
|
|
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease . Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-111191
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment .
|
-
- HY-107625A
-
|
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
|
-
- HY-10081
-
GS-6201
1 Publications Verification
CVT-6883
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) . GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
|
-
- HY-135283
-
|
A-216546
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
|
-
- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
- HY-D0976
-
|
|
P2X Receptor
HIV
|
Infection
|
|
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
|
-
- HY-19996
-
AH-7614
3 Publications Verification
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist .
|
-
- HY-107625
-
|
|
MCHR1 (GPR24)
|
Neurological Disease
Endocrinology
|
|
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
|
-
- HY-124569
-
|
|
iGluR
|
Neurological Disease
|
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
|
-
- HY-14689
-
|
SCH 39166 hydrochloride
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Metabolic Disease
|
|
Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity .
|
-
- HY-14690
-
|
SCH 39166
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Metabolic Disease
|
|
Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity .
|
-
- HY-103149
-
|
SB-216641 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H .
|
-
- HY-119191
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
KF26777 (free base) is a potent and selective adenosine A3 receptor antagonist with an Ki value of 0.2 nM and possesses 9000-, 2350- and 3100-fold selectivity against adenosine A1, A2A and A2B receptors, respectively. KF26777 (free base) potently inhibits the [125I]AB-MECA binding to adenosine A3 receptors. KF26777 (free base) is promising for research of brain ischemia and inflammatory disease including asthma .
|
-
- HY-B1435A
-
|
Thymoxamine
|
Others
|
Neurological Disease
|
|
Moxisylyte (Thymoxamine) is an alpha 1-selective antagonist with activity that improves bladder emptying. Moxisylyte is used to suppress urinary difficulties in patients with multiple system atrophy (MSA) by blocking alpha 1-adrenergic receptors to reduce the amount of residual urine after urination. Moxisylyte is also used to suppress erectile dysfunction and can improve blood circulation problems caused by Raynaud's syndrome in the short term. In addition, Moxisylyte can be applied topically to the eye to reverse the mydriasis caused by phenylephrine and other sympathetic stimulants .
|
-
- HY-111241
-
|
|
Others
|
Neurological Disease
|
|
SV 293 is a selective antagonist with neutral antagonist activity. SV 293 binds to human D2 receptors with 100-fold higher affinity and has lower affinity for human D3 and D4 dopamine receptor subtypes. SV 293 was found to block the effects of the full agonist quinpirole in forskolin-dependent adenylate acylase inhibition assays and electrophysiological assays. SV 293 can be used as a useful pharmacological tool to study the role of dopamine D2-like receptor subtypes in dopamine pathways associated with neurological, neuropsychiatric and movement disorders .
|
-
- HY-150700
-
|
|
ERK
|
Metabolic Disease
|
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
|
-
- HY-107727
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a Ki value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition .
|
-
- HY-B0539S4
-
-
- HY-100449A
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
(S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the
inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R) .
|
-
- HY-B0290
-
-
- HY-18662
-
|
|
TRP Channel
|
Neurological Disease
Cancer
|
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels .
|
-
- HY-B0290A
-
|
ONO-1078 hemihydrate
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-12962
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
|
-
- HY-B0281AS
-
-
- HY-B0309S2
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-122347A
-
|
GW823296 maleate
|
Neurokinin Receptor
|
Neurological Disease
|
|
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
|
-
- HY-12143
-
|
GR 205171A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent .
|
-
- HY-128694
-
|
SR27417
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
|
-
- HY-12598A
-
DHPG
3 Publications Verification
(RS)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs . DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D .
|
-
- HY-106301
-
|
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-130605
-
|
|
P2X Receptor
|
Neurological Disease
|
|
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects .
|
-
- HY-103354A
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities .
|
-
- HY-101418
-
|
|
P2X Receptor
|
Neurological Disease
|
|
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
|
-
- HY-116961
-
-
- HY-123812
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research .
|
-
- HY-P1194
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
|
-
- HY-P1263A
-
-
- HY-136214
-
|
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity .
|
-
- HY-134189A
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
|
-
- HY-111539
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research .
|
-
- HY-11045
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.
PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis .
PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
|
-
- HY-122058A
-
|
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
|
-
- HY-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
- HY-115877
-
|
|
TRP Channel
|
Others
|
|
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma .
|
-
- HY-145572
-
|
LY-3484356
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-10053S1
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
|
-
- HY-14153AS
-
|
SDZ-HTF-919-13C,d3; HTF-919-13C,d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
|
-
- HY-B0309S1
-
|
|
Isotope-Labeled Compounds
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-116248
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
|
-
- HY-103336
-
|
T1117
|
GPR55
Cannabinoid Receptor
|
Cardiovascular Disease
|
|
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
|
-
- HY-145572A
-
|
LY-3484356 tosylate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-136026
-
|
BLU-5937
|
P2X Receptor
|
Inflammation/Immunology
|
|
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
|
-
- HY-10066
-
|
SSR-149415
|
Vasopressin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b Receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca 2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress and anxiety .
|
-
- HY-10635
-
|
|
TRP Channel
|
Inflammation/Immunology
Cancer
|
|
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .
|
-
- HY-18164
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice .
|
-
- HY-B0702R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline (Standard) is the analytical standard of Nicergoline. This product is intended for research and analytical applications. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-101355
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
CGP 20712 is a highly selective β1-adrenoceptor antagonist (Ki=0.3 nmol/L). CGP 20712’s primary mechanism of action is through competitively binding to β1-receptors, thereby blocking the positive chronotropic effects of adrenaline and noradrenaline .
|
-
- HY-B0281AR
-
|
|
Histamine Receptor
Cytochrome P450
Bacterial
|
Infection
Metabolic Disease
Endocrinology
Cancer
|
|
Ranitidine (hydrochloride) (Standard) is the analytical standard of Ranitidine (hydrochloride). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9 .
|
-
- HY-122203A
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-122021
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
J-115814 is a potent and selective neuropeptide Y1 antagonist with Ki values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors .
|
-
- HY-117176
-
|
|
iGluR
|
Neurological Disease
|
|
KRP-199 (compound 14h) is an α-amino-3-hydroxy-5-methylisoxazolepropionic acid receptor (AMPA-R) antagonist (Ki=16 nM) with high potency and selectivity for AMPA-R in vitro and good neuroprotective effects in vivo. KRP-199 can be used in the study of neurodegenerative diseases .
|
-
- HY-17037R
-
|
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-N2600R
-
|
|
Bombesin Receptor
|
Cancer
|
|
Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
|
-
- HY-107626A
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities .
|
-
- HY-118444
-
|
|
Adenosine Receptor
|
Others
|
|
(Rac)-WRC-0571 is a highly potent, orally active and selective, non-xanthine antagonist of A1 adenosine receptors. (Rac)-WRC-0571 inhibits [3H]-N6-cyclohexyladenosine (CHA) binding to guinea pig A1-receptors with a Ki value of 1.1 nM .
|
-
- HY-133166
-
|
|
TRP Channel
|
Neurological Disease
|
|
A-889425 is an oral active selective TRPV1 receptor antagonist with the with an IC50 of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws .
|
-
- HY-B0661C
-
|
YM12617 hydrochloride; LY253351 hydrochloride
|
Others
|
Endocrinology
|
|
Tamsolusin (YM12617) hydrochloride is a highly selective alpha-1A adrenergic receptor antagonist used in the treatment of benign prostatic hypertrophy, demonstrating effective biological activity in alleviating associated symptoms. Tamsolusin hydrochloride can also be quantified using a validated spectrofluorimetric method, showcasing its potential for routine quality control analysis in pharmaceutical formulations.
|
-
- HY-B0411AR
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (monomaleate) (Standard) is the analytical standard of Domperidone (monomaleate). This product is intended for research and analytical applications. Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
|
-
- HY-116941
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
|
-
- HY-103169
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain .
|
-
- HY-110033
-
|
SCH 39166 hydrobromide
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Metabolic Disease
|
|
Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia and obesity .
|
-
- HY-19283
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects .
|
-
- HY-103202A
-
|
|
Others
|
Cardiovascular Disease
|
|
SNAP5089 Free base is a selective α1A-adrenoceptor antagonist with over 1700-fold selectivity for the α1A subtype, which may have implications for the treatment of hypertension and benign prostatic hypertrophy. SNAP5089 demonstrates significant receptor affinity compared to other clinical drugs, emphasizing its potential therapeutic advantages. SNAP5089's high affinity aligns with its suitability for conditions where precise α1A modulation is desirable.
|
-
- HY-76657AR
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
|
-
- HY-18099
-
S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
|
-
- HY-136208
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
|
-
- HY-112461
-
|
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 is a Gsα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
|
-
- HY-106769B
-
|
(3aR,9aR)-GR50360
|
Others
|
Neurological Disease
|
|
(3aR,9aR)-Fluparoxan ((3aR,9aR)-GR50360) is a highly selective and potent α2B adrenaline receptor antagonist with the activity of preventing, improving or inhibiting neurodevelopmental disorders and neurodegenerative diseases. As an α2B receptor antagonist, (3aR,9aR)-Fluparoxan can promote the recovery of neurological function. The mechanism of action of (3aR,9aR)-Fluparoxan makes it have important application potential in neuroscience research .
|
-
- HY-15445
-
CTEP
2 Publications Verification
RO 4956371; mGluR5 inhibitor
|
mGluR
|
Neurological Disease
|
|
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17377
-
|
SCH-417690 maleate; SCH-D maleate
|
CCR
HIV
|
Infection
Endocrinology
Cancer
|
|
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU?570).
|
-
- HY-A0082
-
|
Difenidol hydrochloride
|
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
|
-
- HY-117743S
-
|
|
Isotope-Labeled Compounds
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
|
-
- HY-B0539S2
-
-
- HY-112683
-
|
|
ASCT
|
Cancer
|
|
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells .
|
-
- HY-119217
-
AZ084
2 Publications Verification
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma . AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer .
|
-
- HY-122218
-
JHU-083
4 Publications Verification
|
Glutaminase
|
Neurological Disease
|
|
JHU-083, a proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals .
|
-
- HY-109012
-
|
JNJ-42847922
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
|
-
- HY-107322
-
|
Mepirodipine hydrochloride; YM-09730-5
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-107322A
-
|
Mepirodipine; YM-09730-5 Free base
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-101254
-
|
N-0774
|
Melatonin Receptor
|
Neurological Disease
|
|
Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
|
-
- HY-112683A
-
|
|
ASCT
|
Cancer
|
|
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
|
-
- HY-B1794A
-
|
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
|
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
|
-
- HY-70053A
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
- HY-12294
-
|
NVP-AAM077
|
Caspase
Apoptosis
iGluR
|
Neurological Disease
|
PEAQX (NVP-AAM077) is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
|
-
- HY-107670
-
|
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .
|
-
- HY-P1194A
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
|
-
- HY-P1102A
-
|
|
CXCR
HIV
|
Infection
Cancer
|
|
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
|
-
- HY-P1213A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
|
-
- HY-133529
-
|
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM .
|
-
- HY-120051
-
|
S44819; Egis-13529
|
GABA Receptor
|
Neurological Disease
|
|
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
|
-
- HY-16981
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .
|
-
- HY-19432
-
|
|
iGluR
|
Neurological Disease
|
|
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 .
|
-
- HY-P1213
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
|
-
- HY-B1396S
-
|
BMY-13754-d6; MJ-13754-1-d6
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
|
-
- HY-107712
-
|
|
iGluR
|
Neurological Disease
|
|
TCN 213 is a selective, surmountable, glycine-dependentlly GluN1/GluN2A NMDAR antagonist with IC50s of 0.55, 3.5, 40 μM in the presence of 75, 750, 7500 nM glycine, respectively. TCN 213 can be used to monitor, pharmacologically, the switch in NMDAR expression in developing cortical neurones .
|
-
- HY-108411S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
|
-
- HY-B0640S
-
|
WAL801-13C,d3 hydrobromide
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
|
-
- HY-B1396S1
-
|
BMY-13754-d6 dihydrochloride; MJ-13754-1-d6 dihydrochloride
|
Isotope-Labeled Compounds
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
|
-
- HY-107624
-
ATC0175
1 Publications Verification
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
ATC0175 is a potent, selective and orally active melanin-concentrating hormone 1 recepter antagonist with IC50s of 13.5, >10000 nM for MCH1R, MCH2R, respectively. ATC0175 shows antidepressant effects and anxiolytic effects in animal models. ATC0175 has the potential for the research of depression and/or anxiety disorders .
|
-
- HY-B0203B
-
|
(Rac)-R 065824
|
Adrenergic Receptor
NADPH Oxidase
|
Cardiovascular Disease
|
|
(Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
|
-
- HY-13204B
-
|
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-A0270
-
|
|
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .
|
-
- HY-107656
-
|
|
mAChR
|
Neurological Disease
|
|
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
|
-
- HY-100543
-
|
ICI-118551
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with Ki values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research .
|
-
- HY-15103
-
|
|
PTHR
Androgen Receptor
|
Cancer
|
|
AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) .
|
-
- HY-124160
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for?TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood?brain?barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy .
|
-
- HY-B0192S
-
|
SL 77499-d7
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
|
-
- HY-B0233S1
-
|
PN 200-110-d6
|
Calcium Channel
Autophagy
|
Neurological Disease
|
|
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
|
-
- HY-W062109S
-
|
|
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
|
-
- HY-107707
-
|
|
iGluR
|
Neurological Disease
|
|
TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM . TCS 46b is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-108561
-
|
|
Prostaglandin Receptor
|
Others
|
|
L-670596 is an orally active and selective thrombsxane A2 receptor/prostaglandin receptor antagonist. L-670596 inhibits arachidonic acid (HY-109590) and U-44069 induced bronchoconstriction in the guinea pig. L-670596 also inhibits the aggregation of human platelet rich plasma induced by U-44069 .
|
-
- HY-116076
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety .
|
-
- HY-110099
-
|
|
CXCR
|
Inflammation/Immunology
|
|
(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
|
-
- HY-103209
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Rec 15/2615 hydrochloride is a potent and selective α-1B adrenoceptor antagonist with Ki values of 1.9 nM, 0.3 nM, 2.6 nM for α1A, α1B, α1D, respectively. Rec 15/2615 hydrochloride modulates vaginal smooth muscle contractility and genital engorgement .
|
-
- HY-13204R
-
|
KL 373 hydrochloride (Standard)
|
mAChR
|
Neurological Disease
|
|
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-B0233S2
-
|
PN 200-110-d7
|
Calcium Channel
Autophagy
Isotope-Labeled Compounds
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-13204AR
-
|
|
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-14751R
-
|
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-B0233R
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-117952
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
|
-
- HY-B0192AR
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (hydrochloride) (Standard) is the analytical standard of Alfuzosin (hydrochloride). This product is intended for research and analytical applications. Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-B0309R
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine (Standard) is the analytical standard of Felodipine. This product is intended for research and analytical applications. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier .
|
-
- HY-B2178R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine (difumarate) (Standard) is the analytical standard of Emedastine (difumarate). This product is intended for research and analytical applications. Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-W011245R
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Ranitidine S-oxide (Standard) is the analytical standard of Ranitidine S-oxide. This product is intended for research and analytical applications. Ranitidine S-oxide is the metabolite of Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion .
|
-
- HY-W394717
-
|
PGN 1531
|
Prostaglandin Receptor
PKA
|
Others
|
|
BGC-20-1531 (PGN 1531), a benzenesulfonamide derivative, is a selective EP4 antagonist. BGC-20-1531 binds to PGE2 enhancing the ATPase activity, which are coupled to Gs proteins and thus activate adenylate cyclase generating cAMP and activating PKA. BGC-20-1531 is promising for research of liver disorders .
|
-
- HY-123123
-
|
|
Others
|
Cardiovascular Disease
|
|
RS-61756-007 is a selective thromboxane receptor (TP) agonist with high activity at the TP receptor. RS-61756-007 showed agonism at TP and FP receptors in in vitro studies but had no activity at other receptor subtypes. The effects of RS-61756-007 can be antagonized in a similar manner by the TP antagonist SQ 29,548 .
|
-
- HY-123582
-
|
|
Others
|
Neurological Disease
|
|
CP-866,087 is a novel, potent and selective μ-opioid receptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .
|
-
- HY-19917
-
|
|
Others
|
Neurological Disease
|
|
JNJ-39220675 is a selective and brain-penetrating histamine H3 receptor antagonist with activity in regulating alcohol stimulation and reward. JNJ-39220675 is effective in reducing alcohol intake and preference in alcohol-preferring rats. JNJ-39220675 does not affect the ataxic effects of alcohol, the rate of alcohol elimination, or alcohol-induced nucleocapsid dopamine release .
|
-
- HY-121562
-
|
|
Others
|
Neurological Disease
|
|
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
|
-
- HY-160900
-
|
|
TRP Channel
|
Others
|
|
RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively .
|
-
- HY-19742A
-
|
SRA-333 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Lecozotan (SRA-333) hydrochloride is an orally active and selective antagonist of 5-HT1A with a Ki of 4.5 nM for cloned human 5-HT1A receptor. Lecozotan hydrochloride enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan hydrochloride has the potential for mild-to-moderate Alzheimer's disease (AD) research .
|
-
- HY-50901
-
|
AE 3-208
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer .
|
-
- HY-13200
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
|
-
- HY-10413
-
MK-2894
2 Publications Verification
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .
|
-
- HY-10414
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .
|
-
- HY-76569
-
|
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
Cancer
|
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-16681
-
|
VTP-194310
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively . AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16781
-
|
CJ-023423; RQ-00000007; AAT-007
|
Prostaglandin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [ 3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment [3] .
|
-
- HY-10847A
-
|
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-10046S
-
|
|
Isotope-Labeled Compounds
CXCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
|
Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
|
-
- HY-128345
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP) .
|
-
- HY-103213
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
JP1302 dihydrochloride is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research .
|
-
- HY-12783
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
|
-
- HY-124543
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells . MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-130246
-
|
|
Succinate Receptor 1
|
Inflammation/Immunology
|
|
NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM .
|
-
- HY-14325
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-14325B
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-10656
-
|
|
Urotensin Receptor
|
Inflammation/Immunology
|
|
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
|
-
- HY-100822
-
|
(+)-HA-966
|
iGluR
|
Neurological Disease
|
|
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine . (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain .
|
-
- HY-101333
-
|
(RS)-CPPG
|
mGluR
|
Neurological Disease
|
|
CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors .
|
-
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
-
- HY-14325A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-131945
-
CU-115
2 Publications Verification
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells .
|
-
- HY-13200A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
|
-
- HY-13499
-
|
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
|
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
|
-
- HY-132981
-
|
|
P2X Receptor
|
Neurological Disease
|
|
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .
|
-
- HY-144863
-
|
|
GnRH Receptor
|
Cancer
|
|
BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids .
|
-
- HY-101250
-
|
MDL11939
|
Serotonin Transporter
|
Neurological Disease
|
|
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
|
-
- HY-B0702S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
|
-
- HY-B0693A
-
|
|
Histamine Receptor
Bacterial
SARS-CoV
|
Infection
|
|
Ranitidine bismuth citrate is an orally active Histamine H2-receptor antagonist with an IC50 of 3.3 μM. Ranitidine bismuth citrate has high selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate is a commonly used agent anti-Helicobacter pylori infection with an MIC90 value of 16 ng/L .
|
-
- HY-103204
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia .
|
-
- HY-13206A
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research . MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-103213A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research .
|
-
- HY-13100
-
|
|
Proton Pump
|
Metabolic Disease
|
|
PF 03716556 is a potent, selective, competitive and reversible acid pump (H +,K +-ATPase) antagonist with pIC50s of 6.026, 6.038 and 6.009 for porcine, canine, and human recombinant gastric H +,K +-ATPase, respectively. PF 03716556 is inactive against other receptors, ion channels, and enzymes. PF 03716556 has the potential for gastroesophageal reflux disease research .
|
-
- HY-150270
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
NP-1815-PX is a potent and selective P2X4R antagonist. NP-1815-PX has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
|
-
- HY-150270A
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
NP-1815-PX sodium is a potent and selective P2X4R antagonist. NP-1815-PX sodium has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX sodium also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
|
-
- HY-77111
-
|
|
Others
|
Inflammation/Immunology
Endocrinology
|
|
cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
- HY-15834AR
-
|
SKF-108566J (Standard)
|
Angiotensin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Eprosartan (mesylate) (Standard) is the analytical standard of Eprosartan (mesylate). This product is intended for research and analytical applications. Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-10046R
-
|
|
CXCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
|
Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
|
-
- HY-A0015R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Bepotastine (besilate) (Standard) is the analytical standard of Bepotastine (besilate). This product is intended for research and analytical applications. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-13200B
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BRL-15572 is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
|
-
- HY-124200
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AL 8810 (Item No. 16735) is an 11β-fluoro analog of prostaglandin F2α which acts as a potent and selective antagonist at the FP receptor. AL 8810 isopropyl ester is a lipid soluble, esterified prodrug form of AL 8810 analogous to the commonly used therapeutic intraocular prostaglandin compounds such as Latanoprost (HY-B0577) and Travoprost (HY-B0584).
|
-
- HY-17000R
-
|
|
Vasopressin Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Tolvaptan (Standard) is the analytical standard of Tolvaptan. This product is intended for research and analytical applications. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia .
|
-
- HY-B0567R
-
|
|
Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
|
Infection
Cancer
|
|
Dequalinium (Chloride) (Standard) is the analytical standard of Dequalinium (Chloride). This product is intended for research and analytical applications. Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
|
-
- HY-B1396R
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Nefazodone (hydrochloride) (Standard) is the analytical standard of Nefazodone (hydrochloride). This product is intended for research and analytical applications. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
|
-
- HY-165495
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Pafenolol is a selectively oral-active β1 adrenergic receptor (β1-adrenergic receptor) antagonist that effectively lowers blood pressure. Pharmacokinetic studies in rats indicate that the absorption of Pafenolol is influenced by gastrointestinal contents, with food intake reducing the bioavailability of Pafenolol in rats. Pafenolol can be used in research related to cardiovascular diseases and asthma .
|
-
- HY-B2065
-
|
(-)-Scopolamine hydrochloride; Hyoscine hydrochloride
|
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine hydrochloride is a non-selective and high affinity (≤1 nM) muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. Scopolamine readily passes the blood brain barrier. Scopolamine also reversibly inhibits 5-HT3 receptor-responses with an IC50 of 2.09 μM . Scopolamine induces Alzheimer's disease-like pathology through alteration of cholinergic system .
|
-
- HY-118194
-
|
|
Others
|
Others
|
|
A-65186 is a CCK-A receptor antagonist with the activity of inhibiting CCK8-induced amylase secretion. A-65186 has high binding affinity for pancreatic CCK-A receptors, is more than 500 times more selective for CCK-A receptors than for CCK-B receptors, and can inhibit CCK8-induced amylase secretion.
|
-
- HY-130246A
-
|
|
Succinate Receptor 1
|
Inflammation/Immunology
|
|
NF-56-EJ40 hydrochloride is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 hydrochloride has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM .
|
-
- HY-10895
-
|
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-14604
-
|
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases .
|
-
- HY-103156
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors .
|
-
- HY-101365
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats .
|
-
- HY-101365A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats .
|
-
- HY-112461A
-
|
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
|
-
- HY-B0561
-
|
SC9420
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
- HY-14609
-
|
|
mGluR
|
Neurological Disease
|
|
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14609A
-
MPEP
3 Publications Verification
|
mGluR
|
Neurological Disease
|
|
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17369
-
|
L700462 hydrochloride monohydrate; MK383 hydrochloride monohydrate
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-17369B
-
|
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-16697
-
|
|
GPR55
|
Cancer
|
|
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
|
-
- HY-14348
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities .
|
-
- HY-14405A
-
|
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-132670S
-
|
|
Isotope-Labeled Compounds
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
(R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
|
-
- HY-B0233S
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].
|
-
- HY-110279
-
Ogerin
1 Publications Verification
|
GPR68
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders .
|
-
- HY-N2359
-
|
|
Beta-lactamase
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .
|
-
- HY-12783A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM .
|
-
- HY-135303
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-19578B
-
|
(±)-Isamoltane hemifumarate
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity .
|
-
- HY-B0391B
-
|
KT-611 hydrochloride; BM-15275 hydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia .
|
-
- HY-14485
-
|
|
P2X Receptor
|
Neurological Disease
|
|
Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain .
|
-
- HY-106840
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
|
-
- HY-117829
-
UNC9994
1 Publications Verification
|
Dopamine Receptor
5-HT Receptor
Histamine Receptor
Arrestin
|
Neurological Disease
|
|
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
|
-
- HY-101311
-
|
AIDA
|
mGluR
|
Inflammation/Immunology
Cancer
|
|
UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis .
|
-
- HY-101368A
-
|
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
|
-
- HY-103164
-
|
|
Adenosine Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .
|
-
- HY-107721
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ .
|
-
- HY-101083
-
|
|
Bcl-2 Family
|
Cancer
|
|
BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
|
-
- HY-103413
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent .
|
-
- HY-17369A
-
|
L700462 hydrochloride; MK383 hydrochloride
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) hydrochloride is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-108675
-
|
|
MMP
P2X Receptor
|
Infection
Cancer
|
|
PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers .
|
-
- HY-15008
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor .
|
-
- HY-101188
-
|
|
Histamine Receptor
|
Infection
|
|
INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .
|
-
- HY-106993B
-
|
GT-2331 (enantiomer)
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM) . Cipralisant (enantiomer) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112742
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-14914S1
-
|
TAK-536-d4
|
Apoptosis
Angiotensin Receptor
Reactive Oxygen Species
|
Cancer
|
|
Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].
|
-
- HY-103459
-
|
PD156707
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .
|
-
- HY-A0015A
-
|
|
Others
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-103100
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
SB-699551 is a potent and selective 5-HT5A antagonist with a pKi of 8.3 . SB-699551 inhibits tumorsphere formation. SB-699551 reduces phosphorylation of AKT at serine residue 473 (S473), WNK1, PRAS40. SB-699551 shows anticancer activity and has the potential for the research of breast tumor .
|
-
- HY-107725A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a high affinity for both human and rat Y1 receptors, with IC50 values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-117743S1
-
|
SKF-108566J free base-d6
|
Angiotensin Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-162495
-
|
|
CCR
|
Inflammation/Immunology
|
|
IDOR-1117-2520 is a potent and selective antagonist of CCR6. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 can be used for research of autoimmune diseases .
|
-
- HY-121156
-
|
LF 16-0687; XY-2405
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
|
-
- HY-10119R
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-117743R
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (Standard) is the analytical standard of Eprosartan. This product is intended for research and analytical applications. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-B0002AR
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (hydrochloride dihydrate) (Standard) is the analytical standard of Ondansetron (hydrochloride dihydrate). This product is intended for research and analytical applications. Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery .
|
-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
|
-
- HY-117971
-
|
|
Others
|
Others
|
|
BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
|
-
- HY-12284
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
|
-
- HY-11084
-
|
|
Others
|
Neurological Disease
|
|
SNAP-7941 is a selective antagonist with anxiolytic, antidepressant and appetite suppressant activities. SNAP-7941 showed promising biological activity in initial animal studies. SNAP-7941 targets the melanin concentrating hormone receptor MCH1 and has significant inhibitory potential. SNAP-7941 was shown to inhibit the centrally induced MCH-induced drinking effect in in vivo studies .
|
-
- HY-15007
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists .
|
-
- HY-10895A
-
|
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-18346S
-
|
OPC-31260-d6
|
Isotope-Labeled Compounds
Vasopressin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-10171
-
|
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
|
-
- HY-10007
-
|
SB-262470A
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
|
-
- HY-50101A
-
|
AMD-070 trihydrochloride; AMD-11070 trihydrochloride
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
|
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome .
|
-
- HY-13954
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
- HY-B0391
-
|
KT-611; BM-15275
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
|
-
- HY-100811
-
|
7-CKA
|
iGluR
|
Neurological Disease
|
|
7-Chlorokynurenic acid (7-CKA) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery .
|
-
- HY-100811A
-
|
7-CKA sodium salt
|
iGluR
|
Neurological Disease
|
|
7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid sodium salt is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid sodium salt has potent antinociceptive actions after neuraxial delivery .
|
-
- HY-103178
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
MRE3008F20 is a highly efficient, highly selective and radioactive adenosine A3 receptor (AA3R) antagonist (Ki=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC50 value of 5 nM. MRE3008F20 can be used in the study of AA3R .
|
-
- HY-W010820
-
-
- HY-108676
-
|
|
P2X Receptor
|
Neurological Disease
|
|
NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively .
|
-
- HY-136587
-
|
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
|
-
- HY-B0391A
-
|
KT-611 dihydrochloride; BM-15275 dihydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia .
|
-
- HY-106994A
-
|
YM598
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-108425
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
|
-
- HY-50101
-
|
AMD-070; AMD-11070
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
|
Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Mavorixafor can be used for the study of WHIM syndrome .
|
-
- HY-134188
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
|
-
- HY-B0462S
-
-
- HY-107322S
-
|
Mepirodipine-d5 hydrochloride; YM-09730-5-d5 hydrochloride
|
Isotope-Labeled Compounds
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
|
-
- HY-B0290S1
-
-
- HY-130553
-
|
β-NAAG; β-N-Acetylaspartylglutamic acid
|
Aminopeptidase
mGluR
|
Neurological Disease
|
|
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies .
|
-
- HY-A0030S
-
|
|
mAChR
|
Metabolic Disease
|
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
|
-
- HY-107708
-
|
|
iGluR
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
|
threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity .
|
-
- HY-14914R
-
-
- HY-111291
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats .
|
-
- HY-106838A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Org 6906 is a monoamine reuptake inhibitor that promotes monoaminergic neurotransmission by inhibiting the reuptake of noradrenaline, dopamine, and serotonin. Org 6906 is also an α2 Adrenergic Receptor antagonist, with a pKi value of 6.3 (using the selective α2 adrenergic receptor ligand [ 3H]rauwolscine as a ligand). Org 6906 exhibits antidepressant activity and can be used in research related to neurological disorders .
|
-
- HY-118997
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PD-89211 is a selective dopamine D4 receptor antagonist with a Ki value of 3.7 nM. PD-89211 reverses Quinpirole (HY-B1752A)-induced [3H]thymidine uptake in CHOpro5 cells (IC50 = 2.1 nM). PD-89211 regulates dopamine/norepinephrine metabolism in the hippocampus and can be used for research on central nervous system disorders such as schizophrenia .
|
-
- HY-114076
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .
|
-
- HY-14483A
-
|
Ro-4 hydrochloride
|
P2X Receptor
|
Cancer
|
|
AF-353 hydrochloride is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3 .
|
-
- HY-10119AR
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-A0030R
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-121129
-
|
FLB-131
|
Dopamine Receptor
|
Neurological Disease
|
|
Eticlopride, a potent and selective D2 receptor antagonist, was investigated in rats with extensive dopamine denervation induced by 6-hydroxydopamine. Daily injections of eticlopride over 21 days increased D2 receptor density in intact brain regions but did not further augment already increased densities in denervated areas. Despite receptor density changes, functional sensitivity remained evident, as shown by contralateral rotations induced by D2 agonist quinpirole during wash-out periods. The study suggests that chronic D2 receptor blockade and dopamine denervation may share a common mechanism in upregulating D2 receptor density, contrary to previous reports suggesting additive effects of denervation and antagonist treatment .
|
-
- HY-50101C
-
|
AMD-070 hydrochloride; AMD-11070 hydrochloride
|
CXCR
HIV
|
Infection
Cancer
|
|
Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 nM and 9 nM, respectively. Mavorixafor hydrochloride can be used for the study of WHIM syndrome .
|
-
- HY-124117
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors .
|
-
- HY-13315
-
|
MK0476
|
Leukotriene Receptor
|
Inflammation/Immunology
Cancer
|
|
Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research .
|
-
- HY-B0480
-
|
(±)-Brompheniramine maleate
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-100619
-
|
AM152
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist . BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively . BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-101189
-
|
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
|
-
- HY-16023A
-
|
EM-652; SCH 57068
|
Estrogen Receptor/ERR
|
Cancer
|
|
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
|
-
- HY-101478
-
|
|
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
|
-
- HY-135594
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A .
|
-
- HY-135595
-
|
|
Estrogen Receptor/ERR
Drug Metabolite
|
Metabolic Disease
|
|
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A .
|
-
- HY-117958
-
HJC0197
1 Publications Verification
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP .
|
-
- HY-106994
-
|
YM598 free base
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-18596
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively . SB-215505 increases wakefulness and motor activity in rats .
|
-
- HY-101189B
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
|
-
- HY-101222
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-103155
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease .
|
-
- HY-103094
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
|
-
- HY-103135
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT2B / 5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92) . SB 206553 possesses anxiolytic-like properties .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
|
-
- HY-B0480A
-
-
- HY-147336
-
|
|
Drug Metabolite
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
|
-
- HY-14539
-
|
HF 1854
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-103277
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-17037S1
-
|
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
|
Cancer
|
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-100672B
-
|
|
Others
|
Cardiovascular Disease
Metabolic Disease
|
|
(2R)-SR59230A is the isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively .
|
-
- HY-103277A
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
-
- HY-110056
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 hydrochloride is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects .
|
-
- HY-101478A
-
|
|
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
|
-
- HY-106982
-
|
CJ-11,974
|
Neurokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research .
|
-
- HY-106301R
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-B0290R
-
|
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast (Standard) is the analytical standard of Pranlukast. This product is intended for research and analytical applications. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-14539A
-
|
HF 1854 hydrochloride
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-116723
-
|
|
mGluR
|
Neurological Disease
|
|
CFMMC is a selective allosteric metabotropic glutamate receptor 1 (mGluR1) antagonist. CFMMC inhibits L-glutamate-induced intracellular Ca 2+ mobilization ([Ca 2+]i) in Chinese hamster ovary cells expressing recombinant human mGluR1a with an IC50 value of 50 nM. CFMMC is promising for research of various central nervous system disorders, such as schizophrenia, epilepsy, anxiety, pain, cognitive dysfunction and drug abuse .
|
-
- HY-122215
-
|
N-696
|
Others
|
Endocrinology
|
|
Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
|
-
- HY-135507A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NAS181 free base is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors .
|
-
- HY-70050A
-
|
GR 68755; GR 68755X
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-70050C
-
|
GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-B0135
-
|
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl -?(NKCC) cotransporter, NKCC1 and NKCC2 .?Furosemide is also a GABAA?receptors antagonist and displays 100-fold selectivity for?α6-containing receptors than?α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-B0135A
-
|
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-B0002B
-
|
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
|
-
- HY-12294A
-
|
NVP-AAM077 tetrasodium hydrate
|
Apoptosis
Caspase
iGluR
|
Neurological Disease
|
PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a tetrasodium hydrate of PEAQX (HY-12294). PEAQX tetrasodium hydrate is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX tetrasodium hydrate can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
|
-
- HY-B1081
-
|
6-Hydroxydopamine Hydrochloride
|
Dopamine Receptor
Autophagy
Mitophagy
COX
PGE synthase
Interleukin Related
p38 MAPK
Apoptosis
Caspase
|
Neurological Disease
Cancer
|
|
Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome .
|
-
- HY-14483
-
AF-353
1 Publications Verification
Ro-4
|
P2X Receptor
|
Cancer
|
|
AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3 .
|
-
- HY-101986
-
|
AR-H 053591
|
Neuropeptide Y Receptor
|
Metabolic Disease
Endocrinology
|
|
BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [ 125I]PYY3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy .
|
-
- HY-B1901
-
|
(±)-Eperisone hydrochloride
|
Others
|
Neurological Disease
|
|
Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
|
-
- HY-103154
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects .
|
-
- HY-100277
-
|
SR-202
|
PPAR
|
Metabolic Disease
|
|
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-100943
-
|
SQ 10643
|
5-HT Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro .
|
-
- HY-125957
-
|
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM) and myosin light chain kinase (MLCK) (Ki=7.4 μM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively .
|
-
- HY-124748A
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
|
ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis .
|
-
- HY-13315A
-
|
MK0476 free base
|
Leukotriene Receptor
|
Inflammation/Immunology
Cancer
|
|
Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research .
|
-
- HY-121392
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .
|
-
- HY-P2264
-
|
|
Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
|
-
- HY-141513
-
NH-3
3 Publications Verification
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment . NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14327
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic .
|
-
- HY-103450
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-110152
-
|
|
mGluR
|
Neurological Disease
|
|
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17366
-
|
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-17366A
-
|
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-101986A
-
|
AR-H 053591 hydrochloride
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [ 125I]PYY3-36. BIIE-0246 hydrochloride decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 hydrochloride reduces albuminuria in ADR nephropathy .
|
-
- HY-P1130
-
|
Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is a selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits Ki values of 13.1 nM and 420 nM for GalR2 and GalR1, respectively. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain) .
|
-
- HY-124748
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
|
ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis .
|
-
- HY-164083
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR65630 is a potent and selective 5-hydroxytryptamine (5-HT) type 3 receptor antagonist. GR65630 can be used to study the expression patterns of 5-HT3 receptors in different brain regions and their possible functions in the central nervous system. GR65630 and its radiolabeled form [ 3H]GR65630 can be used to study the distribution, density and affinity of the receptors .
|
-
- HY-159584
-
|
|
iGluR
|
Neurological Disease
|
|
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
|
-
- HY-A0082R
-
|
|
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
|
-
- HY-118758
-
|
γ-Kainic acid-glutamic acid
|
Sodium Channel
|
Neurological Disease
|
|
γ-Kainylglutamic acid (γ-Kainic acid-glutamic acid), a dipeptide derived from kainic and L-Glutamic acids, is a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties. γ-Kainylglutamic acid inhibits the stimulation of Na + fluxes induced in brain slices by the neuroexcitant N-methyl-D-aspartic acid. γ-Kainylglutamic acid is also effective in protecting mice from picrotoxin-induced convulsions with an EC50 value of 0.17 μmol .
|
-
- HY-167704
-
|
|
Others
|
Cancer
|
|
NF023 is a compound that inhibits X-BIR1/TAB1 assembly activity. NF023 can affect cell survival signaling pathways by interfering with XIAP-mediated NF-κB activation. NF023 also shows potential as a selective P2X1 adenylate receptor antagonist. This compound has the potential to synergize with existing pro-apoptotic drugs and play an important role in cancer suppression .
|
-
- HY-103430
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-103430A
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-19633A
-
|
|
Others
|
Neurological Disease
|
|
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
|
-
- HY-P1320
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
![[Nphe1]Nociceptin(1-13)NH2](//file.medchemexpress.eu/product_pic/hy-p1320.gif)
- HY-P1320A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
![[Nphe1]Nociceptin(1-13)NH2 TFA](//file.medchemexpress.eu/product_pic/hy-p1320a.gif)
- HY-U00237B
-
|
|
Others
|
Others
|
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-A0033
-
|
UK-88525
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-13285
-
|
Debio 0719
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
|
-
- HY-13527
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HTSumatriptan (HY-B0121B)-induced decrease in excitatory postsynaptic potential (EPSC) amplitude .
|
-
- HY-13508
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .
|
-
- HY-14564A
-
|
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
|
-
- HY-B1081A
-
|
6-Hydroxydopamine hydrobromide; 6-OHDA hydrobromide
|
Dopamine Receptor
Autophagy
Mitophagy
COX
PGE synthase
Interleukin Related
p38 MAPK
Apoptosis
Caspase
|
Neurological Disease
Cancer
|
|
Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome .
|
-
- HY-15102
-
MK-0429
3 Publications Verification
L-000845704
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
|
-
- HY-P1454
-
Fz7-21
3 Publications Verification
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs the function of FZD7 in Wnt–β-catenin signalling and stem cell function in intestinal organoids .
|
-
- HY-105685
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .
|
-
- HY-125028
-
|
|
Src
HIV
|
Infection
|
|
Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-18618
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-139567
-
|
BMS-986256
|
Toll-like Receptor (TLR)
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus) .
|
-
- HY-18618A
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-D0014
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
|
-
- HY-108656
-
|
|
P2Y Receptor
Arrestin
|
Cardiovascular Disease
|
|
MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors .
|
-
- HY-103174
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment . MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0391S1
-
|
KT-611-d5; BM-15275-d5
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
|
-
- HY-13315B
-
|
MK0476 dicyclohexylamine
|
Leukotriene Receptor
|
Inflammation/Immunology
Cancer
|
|
Montelukast (MK0476) dicyclohexylamine is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast dicyclohexylamine can be used for the reseach of asthma and liver injury. Montelukast dicyclohexylamine also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast dicyclohexylamine decreases eosinophil infiltration into the asthmatic airways. Montelukast dicyclohexylamine can also be used for COVID-19 research .
|
-
- HY-101170
-
|
|
Imidazoline Receptor
Apoptosis
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .
|
-
- HY-148494
-
|
FLX475
|
CCR
|
Inflammation/Immunology
Cancer
|
Tivumecirnon (FLX475) is an orally bioactive, selective CCR4 antagonist. Tivumecirnon can block the recruitment of immunosuppressive regulatory T cells (Treg) into the tumor microenvironment, leading to enhanced antitumor activity. Tivumecirnon has antitumor activity on EBV+ NK/T cell lymphoma and non-small cell lung cancer (NSCLC) combined with Pembrolizumab (HY-P9902). Tivumecirnon is promising for research of broad range of tumor types .
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-
- HY-148502
-
|
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mAChR
|
Neurological Disease
|
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
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-
- HY-117133
-
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SF0166
|
Integrin
|
Metabolic Disease
|
|
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
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-
- HY-12706
-
-
- HY-19989
-
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L-660711
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
|
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
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-
- HY-106837
-
|
Y 24180
|
Platelet-activating Factor Receptor (PAFR)
|
Inflammation/Immunology
|
|
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+ influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice .
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- HY-107322AS1
-
|
Mepirodipine-d5; YM-09730-5-d5 Free base
|
Isotope-Labeled Compounds
|
Others
|
|
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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-
- HY-103378
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects .
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-
- HY-76569S1
-
|
PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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-
- HY-17369BR
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (Standard) is the analytical standard of Tirofiban. This product is intended for research and analytical applications. Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
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-
- HY-17369R
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (hydrochloride monohydrate) (Standard) is the analytical standard of Tirofiban (hydrochloride monohydrate). This product is intended for research and analytical applications. Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
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-
- HY-76569R
-
|
|
mAChR
|
Neurological Disease
|
|
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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-
- HY-19202
-
|
rac-EMA401; rac-PD-126055; EMA400
|
Angiotensin Receptor
|
Neurological Disease
|
|
rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT2 receptor antagonist with IC50s of 75.2 nM and 2918 nM for AT2R and AT1R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve .
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-
- HY-117053
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ 3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ 3H]NKA to cloned human NK-2R .
|
-
- HY-115375
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
50595 hydrochloride is a selective noncompetitive cisapride antagonist that interferes with the activity of cisapride and BRL 24924. R 50595 hydrochloride has no effect on the response to electrical stimulation at concentrations up to 3 X 10(-7) M. R 50595 hydrochloride antagonizes the effects of cisapride and BRL 24924 in a noncompetitive manner. R 50595 hydrochloride completely abolishes the effects of 5-HT at a concentration of 3 X 10(-7) M and also antagonizes the effects of 5-HT in a noncompetitive manner .
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-
- HY-117637
-
|
|
Others
|
Neurological Disease
|
|
ALS-I-41 is a novel, potent and selective oxytocin receptor antagonist with the potential to modulate biological activities related to social behavior and mental disorders. ALS-I-41 is being evaluated for behavioral pharmacology experiments in non-human primates and can be administered via intranasal or intramuscular injection. The central nervous system penetration and metabolic rate of ALS-I-41 were studied by mass spectrometry analysis in cerebrospinal fluid and plasma of macaque monkeys .
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-
- HY-103556
-
|
|
mGluR
|
Neurological Disease
|
|
YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity and neuroprotective properties in vivo. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki value of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 value of 8.6 nM. YM-202074 fumarate can be used in stroke research .
|
-
- HY-15724
-
|
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
|
-
- HY-10847B
-
|
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate?dopamine D3?receptor (D3R)?antagonist with Ki values of 10.7?nM and?11.2 nM?at?rodent and human?D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with?pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
|
-
- HY-15724A
-
|
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
|
-
- HY-A0012
-
|
UK-88525 hydrobromide
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-15342
-
|
OC000459
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils .
|
-
- HY-B0539
-
|
Sch34117
|
Histamine Receptor
TNF Receptor
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria .
|
-
- HY-13106
-
|
EMA401; PD-126055; (S)-EMA400
|
Angiotensin Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-10349A
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist .
|
-
- HY-112611
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations .
|
-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-15342A
-
|
OC000459 sodium
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils .
|
-
- HY-P1454A
-
|
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 TFA impairs the function of FZD7 in Wnt-β-catenin signalling and stem cell function in intestinal organoids .
|
-
- HY-P1106
-
|
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study .
|
-
- HY-18617
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-123857
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .
|
-
- HY-107615
-
|
|
LPL Receptor
|
Cancer
|
|
TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets . TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells .
|
-
- HY-119101
-
|
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
|
-
- HY-126037
-
|
|
ROR
|
Inflammation/Immunology
|
|
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
|
-
- HY-110126
-
|
|
P2Y Receptor
|
Inflammation/Immunology
Cancer
|
|
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth .
|
-
- HY-13106A
-
|
EMA401 sodium; PD-126055 sodium
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
|
Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-19858
-
|
|
iGluR
|
Neurological Disease
|
|
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
|
-
- HY-N12422
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research .
|
-
- HY-14539R
-
|
HF 1854 (Standard)
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-13315R
-
|
MK0476 (Standard)
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Montelukast (sodium) (Standard) is the analytical standard of Montelukast (sodium). This product is intended for research and analytical applications. Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research .
|
-
- HY-B0391R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Naftopidil (Standard) is the analytical standard of Naftopidil. This product is intended for research and analytical applications. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
|
-
- HY-133828
-
|
|
5-HT Receptor
SARS-CoV
|
Infection
|
|
Cinanserin (SQ 10643) is a potent and selective 5-HT2 antagonist with Ki values of 41, 3500 nM for 5-HT2, 5-HT1, respectively. Cinanserin also is a SARS-CoV 3CL pro inhibitor with an KD value of 49.4, 18.2 µM for SARS-CoV 3CL pro, HCoV-229E 3CL pro, respectively. Cinanserin reduces systemic burn edema levels .
|
-
- HY-B0480R
-
|
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-101349
-
|
|
Dopamine Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
L 741742 is a dopamine receptor D4 (DRD4) antagonist that selectively inhibits glioblastomas (GBM) growth in vitro and in vivo, synergyed with Temozolomide (TMZ) (HY-17364). L 741742 disrupts in effectors PDGFRβ/ERK1/2 and mTOR signaling. Additionally, L 741742 disrupts endolysosmal function compromising the autophagy-lysosomal degradation pathway, followed by G0/G1 cell cycle arrest and Apoptosis. L 741742 is promising for research of GBM and neurogenesis .
|
-
- HY-114539
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-750667 triHydrochloride is a selective antagonist for the D4 dopamine receptor, with a Ki value of 0.51 nM. The radiolabeled form of L-750667, [ 125I]L-750,667, has a Kd value of 0.16 nM for the D4 receptor. L-750667 triHydrochloride can reverse dopamine-induced inhibition of cAMP accumulation. It can be used to study the distribution and function of D4 dopamine receptors in the central nervous system and has potential applications in the fields of neuroscience and psychiatry .
|
-
- HY-100481
-
|
RPR101048
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
|
-
- HY-B0480AR
-
|
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Brompheniramine (Standard) is the analytical standard of Brompheniramine. This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research [4].
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-
- HY-107510
-
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mGluR
|
Neurological Disease
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|
YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
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- HY-136587R
-
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Histamine Receptor
mGluR
|
Inflammation/Immunology
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Oxomemazine (Standard) is the analytical standard of Oxomemazine. This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
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- HY-10564
-
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MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
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Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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- HY-122575
-
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P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
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- HY-100539
-
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Others
|
Others
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PD 128907 is a D3 receptor ligand with activities of activating dopamine receptors, inhibiting cell firing, and inhibiting dopamine release. The active (+) enantiomer of PD 128907 has high affinity and selectivity for rat D3 dopamine receptors. PD 128907 inhibits cell firing in the ventral tegmental area and substantia nigra pars compacta with EC50 values of 33nM and 38nM, respectively. PD 128907 also inhibits dopamine release in the caudate putamen with an EC50 of 66nM. However, the selective D2 receptor antagonist L-741,626 has high affinity for receptors activated by PD 128907, indicating that the effects of PD 128907 are more likely on D2 autoreceptors rather than D3 dopamine receptor subtypes.
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- HY-B0203BS2
-
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(Rac)-R 065824-d2,15N
|
NADPH Oxidase
Adrenergic Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
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(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
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- HY-B0725
-
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Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
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Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
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- HY-19989A
-
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L-660711 sodium
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
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MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
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- HY-100588
-
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mGluR
|
Neurological Disease
|
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VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
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- HY-106993
-
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GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
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Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-14850
-
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Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
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Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM . Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively .
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- HY-B0135S
-
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NKCC
GABA Receptor
|
Metabolic Disease
Cancer
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Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].
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-
- HY-136242
-
|
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Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
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UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
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-
- HY-100588A
-
|
|
mGluR
|
Neurological Disease
|
|
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
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-
- HY-101249
-
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Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .
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-
- HY-108672
-
|
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P2Y Receptor
|
Inflammation/Immunology
|
|
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively . NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA) .
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-
- HY-114208A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
|
-
- HY-119293
-
K777
1 Publications Verification
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
|
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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-
- HY-103129A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo .
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-
- HY-103129
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo .
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-
- HY-P1106A
-
|
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CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study .
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-
- HY-112146
-
MMG-11
2 Publications Verification
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses .
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- HY-112146A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses .
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-
- HY-114208
-
|
|
Histone Methyltransferase
|
Cancer
|
|
BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
|
-
- HY-B1562
-
|
(±)-Bopindolol
|
Adrenergic Receptor
Renin
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
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-
- HY-106993A
-
|
GT-2331 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-120802
-
|
AZD-8871; LAS191351
|
mAChR
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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-
- HY-B1562C
-
|
(±)-Bopindolol fumarate
|
Adrenergic Receptor
Renin
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
|
-
- HY-100449
-
|
|
Prostaglandin Receptor
p38 MAPK
ERK
|
Neurological Disease
Endocrinology
|
|
AL-8810 is a potent and selective antagonist of the PGF 2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The Ki of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG) .
|
-
- HY-12709A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARC 239 dihydrochloride is a selective α2B/2C adrenoceptor antagonist (pKd values are 5.95, 7.41 and 7.56 at α2A, α2B, and α2C receptors respectively). ARC 239 dihydrochloride binds to CHO cell membranes expressing human recombinant a2A-, a2B- or a2C-adrenoceptor subtypes with pKis of 5.6, 8.4, and 7.08, respectively .
|
-
- HY-148825
-
-
- HY-123468
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-101083A
-
|
|
Bcl-2 Family
|
Cancer
|
|
(Rac)-BDA-366 (example 2) is the despinner of BDA-366 (HY-101083). BDA-366 is a potent Bcl-2 antagonist (Ki=3.3 nM), binding Bcl-2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl-2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
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-
- HY-B0135R
-
|
|
NKCC
GABA Receptor
|
Metabolic Disease
Cancer
|
|
Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-70050CR
-
|
GR 68755C (Standard); GR 68755 Hydrochloride (Standard); GR 68755X Hydrochloride (Standard)
|
5-HT Receptor
|
Neurological Disease
|
|
Alosetron (Hydrochloride) (Standard) is the analytical standard of Alosetron (Hydrochloride). This product is intended for research and analytical applications. Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-100277R
-
|
|
PPAR
|
Metabolic Disease
|
|
Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-13315AR
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Montelukast (Standard) is the analytical standard of Montelukast. This product is intended for research and analytical applications. Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research .
|
-
- HY-B0002BR
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (Standard) is the analytical standard of Ondansetron. This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
|
-
- HY-P10429
-
|
|
CXCR
|
Infection
|
|
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
|
-
- HY-117792
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
LY314228 is an aminoguanidine 5-HT2 antagonist with relative selectivity for 5-HT2A receptors (IC50: 147.9 nM). The Ki values ??of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .
|
-
- HY-123244
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
YC137 is a potent Bcl-2 antagonist with Kis of 1.3 μM and >100 μM for Bcl-2 and Bcl-xL when assayed in Bis-Tris buffer, respectively. YC137 inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2. YC137 selectively induces apoptosis of Bcl-2-dependent cells. YC137 has the potential for breast cancer research .
|
-
- HY-117694
-
|
|
CGRP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine .
|
-
- HY-106909A
-
|
KAE-393
|
5-HT Receptor
|
Cardiovascular Disease
|
|
YM114 (KAE-393) is a highly potent and selective (5-HT)3-receptor antagonist that does not affect Veratridine (HY-N6691)- or electrical stimulation-induced bradycardia in anesthetized rats. YM114 inhibits 2-methyl-5-HT (HY-19358)-induced Bezold-Jarisch reflex, which originates from (5-HT)3-receptor located on the endings of vagal afferent nerves in the heart .
|
-
- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-109139A
-
|
NIR178 mesylate; PBF509 mesylate
|
Adenosine Receptor
|
Cancer
|
|
Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA .
|
-
- HY-119293A
-
|
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
|
K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
|
-
- HY-111198
-
|
|
Others
|
Inflammation/Immunology
|
|
YM-355179 fumarate is a newly synthesized selective CCR3 antagonist with the potential to inhibit eosinophil-related allergic inflammatory diseases. YM-355179 can effectively inhibit the binding of CCL11 and CCL5 to CCR3-expressing cells, with IC50 values of 7.6 nM and 24 nM respectively. In functional experiments, YM-355179 can inhibit CCL11-induced intracellular Ca(2+) influx, chemotaxis and eosinophil degranulation, IC50 The values are 8.0 nM, 24 nM and 29 nM respectively .
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-
- HY-136659
-
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Others
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Others
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|
Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .
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- HY-14541A
-
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LY170053 hydrochloride
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic .
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-
- HY-15568
-
|
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P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
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-
- HY-15568A
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
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- HY-10564S
-
|
MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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-
- HY-136693
-
|
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Others
|
Neurological Disease
|
|
L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
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-
- HY-112348
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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-
- HY-17038
-
|
S-20098
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
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-
- HY-17038A
-
|
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
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-
- HY-100186
-
|
|
Androgen Receptor
|
Cardiovascular Disease
Others
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
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-
- HY-10965
-
|
KW-3902
|
Adenosine Receptor
|
Neurological Disease
|
|
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
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-
- HY-14994
-
|
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Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
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-
- HY-111828
-
TTA-A2
1 Publications Verification
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy .
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-
- HY-120802A
-
|
AZD-8871 saccharinate; LAS191351 saccharinate
|
mAChR
Adrenergic Receptor
|
Infection
Inflammation/Immunology
|
|
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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-
- HY-14993
-
|
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Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
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-
- HY-B1562B
-
|
(±)-Bopindolol (malonate)
|
Adrenergic Receptor
Renin
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
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-
- HY-14541
-
|
LY170053
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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-
- HY-106954
-
|
Rec 15/2739; Recordati 15/2739; SB 216469
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction .
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-
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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-
- HY-A0012R
-
|
UK-88525 (hydrobromide) (Standard)
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
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-
- HY-163436
-
|
|
FXR
Cytochrome P450
RAR/RXR
PPAR
ROR
|
Metabolic Disease
|
|
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders .
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-
- HY-14564
-
|
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .
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-
- HY-123567
-
|
|
Others
|
Neurological Disease
|
|
LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
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-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-N7536
-
|
|
TRP Channel
|
Others
|
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
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-
- HY-167848
-
|
XL-118
|
Others
|
Cardiovascular Disease
|
|
DMP-728 free base (XL-118) is a highly potent and selective GPIIb/IIIa antagonist with antiplatelet and antithrombotic activities. DMP-728 free base can inhibit ADP-induced human platelet aggregation in vitro, with an IC50 of 46 nmol/L, and can significantly reduce the interaction between fibrinogen and human platelets or Binding of purified human GPIIb/IIIa receptors. DMP-728 free base exhibits dose-dependent antiplatelet effects in anesthetized mongrel dogs, effectively inhibiting ADP-induced platelet aggregation and prolonging template bleeding time .
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-
- HY-13315BR
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
Cancer
|
|
Montelukast (dicyclohexylamine) (Standard) is the analytical standard of Montelukast (dicyclohexylamine). This product is intended for research and analytical applications. Montelukast (MK0476) dicyclohexylamine is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast dicyclohexylamine can be used for the reseach of asthma and liver injury. Montelukast dicyclohexylamine also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast dicyclohexylamine decreases eosinophil infiltration into the asthmatic airways. Montelukast dicyclohexylamine can also be used for COVID-19 research .
|
-
- HY-70050
-
|
GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-70050B
-
|
GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-13409
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
|
-
- HY-13409A
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
|
-
- HY-B1213
-
|
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
|
-
- HY-19975
-
|
|
TRP Channel
|
Neurological Disease
Cancer
|
|
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) . RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells .
|
-
- HY-N4267
-
|
|
Calcium Channel
|
Infection
Cardiovascular Disease
|
|
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
|
-
- HY-101044
-
|
|
P2X Receptor
Na+/Ca2+ Exchanger
|
Neurological Disease
|
|
PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca 2+ exchanger in guinea pig airway smooth muscle .
|
-
- HY-111052
-
|
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
|
-
- HY-17038B
-
|
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-100794
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
|
-
- HY-B1213A
-
|
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
|
-
- HY-147319
-
|
|
Others
|
Neurological Disease
|
|
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
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-
- HY-107664
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
|
-
- HY-107664A
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
|
-
- HY-157998
-
|
|
mGluR
Src
|
Others
|
|
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
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-
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a selective D1-D2 heterogeneous antagonist. TAT-D1 peptide destroys the heterodimer of the D1-D2 receptor by interacting with the specific domain of the D2 receptor through its unique amino acid sequence, in particular the two glutamate residues at the C terminal of the D1 receptor. TAT-D1 peptide can be used to study the role of D1-D2 receptor heterodimers in the regulation of depressive and anxiety-like behaviors .
|
-
- HY-136702
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
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-
- HY-101317A
-
|
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
|
-
- HY-17038S1
-
|
S-20098-d4
|
Isotope-Labeled Compounds
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
|
-
- HY-17038S2
-
|
S-20098-d3
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
|
-
- HY-19306
-
|
|
Integrin
|
Cancer
|
|
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression .
|
-
- HY-108511A
-
|
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
|
|
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
|
-
- HY-W009009
-
|
|
GABA Receptor
|
Neurological Disease
|
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
|
-
- HY-101308
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
|
-
- HY-101308A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
|
-
- HY-108511
-
|
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
|
|
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
|
-
- HY-B0822S1
-
|
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-P99483
-
|
AT 004; VT 007
|
CD20
Adenosine Receptor
|
Cancer
|
|
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .
|
-
- HY-14541R
-
|
LY170053 (Standard)
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-B0725R
-
|
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-17038R
-
|
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-19927A
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
|
-
- HY-W052508
-
|
N-Desalkylquetiapine
|
5-HT Receptor
|
Neurological Disease
|
|
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
|
-
- HY-117380
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
|
-
- HY-14541S2
-
|
LY170053-d8
|
Isotope-Labeled Compounds
Apoptosis
Dopamine Receptor
Autophagy
mAChR
Mitophagy
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-12191
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation .
|
-
- HY-15074
-
|
NS-1209
|
iGluR
|
Neurological Disease
|
|
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
|
-
- HY-18200A
-
|
E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
|
-
- HY-13409B
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 monohydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 monohydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 monohydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
|
-
- HY-15076
-
|
NS-1209 sodium
|
iGluR
|
Neurological Disease
|
|
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
|
-
- HY-118935
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
NGD9002 free base is a new generation of selective corticotropin-releasing factor-1 (CRF-1) receptor antagonist with inhibitory activity on CRF-induced colonic function stimulation. NGD9002 free base can reduce CRF-induced fecal output response and show an inhibitory IC50 value of 4.3 mg/kg. NGD9002 free base can effectively block CRF-induced colonic secretory motility stimulation at the highest dose and reduce acute water avoidance-induced defecation. NGD9002 free base can also prevent the occurrence of pain hypersensitivity reactions to repeated colonic distension .
|
-
- HY-19545A
-
|
R-(+)-SCH-23390 hydrochloride
|
Dopamine Receptor
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
|
-
- HY-107018
-
|
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- HY-108400
-
|
R-(+)-SCH-23390 maleate
|
Dopamine Receptor
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
|
-
- HY-122197
-
|
|
CXCR
Apelin Receptor (APJ)
Arrestin
|
Cancer
|
|
ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research .
|
-
- HY-101343
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
|
-
- HY-100554
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
|
-
- HY-162677
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
|
-
- HY-19974
-
TAK-220
2 Publications Verification
|
CCR
HIV
|
Infection
Endocrinology
|
|
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
|
-
- HY-102093A
-
|
|
Others
|
Others
|
|
ZD 7155 is an AT1R selective antagonist with renal function modulating activity. The effects of ZD 7155 on glomeruli and tubules were measured in 1- (N = 9) and 6-week-old (N = 13) lambs. Pretreatment with ZD 7155 after L-NAME infusion did not alter glomerular function in 1- or 6-week-old lambs. During postnatal development, Ang II modulates the effects of NO on electrolyte handling via AT1R and AT2R. In 6-week-old lambs, selective inhibition of AT1R and AT2R increased the excretion of Na+, K+, and Cl-. In 6-week-old lambs, pretreatment with ZD 7155 and PD 123319 followed by the addition of L-NAME increased urine flow rate by 200%, free water clearance by 50%, and decreased urine osmolality by 40%. The same trends of changes in these variables were also observed when L-NAME was added to ZD 7155 or PD 123319, although to a lesser extent.
|
-
- HY-19978
-
|
|
P2X Receptor
|
Neurological Disease
|
|
RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7) .
|
-
- HY-101009
-
|
Metitepine maleate; Ro-8-6837 maleate
|
5-HT Receptor
|
Neurological Disease
|
|
Methiothepin maleate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-B1213R
-
|
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine (maleate) (Standard) is the analytical standard of Trimipramine (maleate). This product is intended for research and analytical applications. Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
|
-
- HY-111491
-
|
Metitepine; Ro 8-6837
|
5-HT Receptor
|
Neurological Disease
|
|
Methiothepin is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-117881
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
|
-
- HY-B1213AR
-
|
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
|
-
- HY-107836
-
|
Metitepine mesylate; Ro 8-6837 mesylate
|
5-HT Receptor
|
Neurological Disease
|
|
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-P1110
-
AF12198
1 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
|
-
- HY-103211
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
|
-
- HY-12716
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
BRL-44408 is a selective adrenergic receptor antagonist of α2A/α2B AR. BRL-44408 can effectively antagonize the inhibitory effects of norepinephrine or adrenergic receptor agonist Clonidine (HY-12721) on K +-induced [3H]norepinephrine and [3H]5-hydroxytryptamine release. BRL-44408 has a higher affinity for human platelet membranes containing α2A-adrenoceptors than BRL-41992 and Imiloxan (HY-101337). BRL-44408 may affect the release of norepinephrine and 5-hydroxytryptamine through a mechanism mediated by α2A-adrenoceptors, and has a potential role in the regulation of neurotransmitter release .
|
-
- HY-164552
-
|
|
Apoptosis
Androgen Receptor
|
Cancer
|
|
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
|
-
- HY-N2037
-
|
Norcoclaurine; Demethyl-Coclaurine
|
MAP3K
MDM-2/p53
Adrenergic Receptor
ROS Kinase
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-103117
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis=6.6 and 8.9 nM, respectively). It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor (Ki=5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s=38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s=38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D0014
-
|
|
Indicators
|
|
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-151413
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
|
-
- HY-P1782
-
-
- HY-P0209
-
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
-
- HY-P3854
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
|
-
- HY-P1018
-
-
- HY-P2669
-
-
- HY-105436
-
-
- HY-P1681
-
-
- HY-P1017
-
-
- HY-12488
-
LY2510924
Maximum Cited Publications
12 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
|
LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
|
-
- HY-P1194B
-
-
- HY-P3227
-
|
XJ735
|
Integrin
|
Inflammation/Immunology
|
|
Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertension
Research .
|
-
- HY-P10473
-
-
- HY-P1276
-
|
Neurokinin-2 receptor antagonist
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
|
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-P3213
-
-
- HY-P5111
-
|
|
Peptides
|
Neurological Disease
|
|
Myristoyl-(Lys12,27,28)-VIP-Gly-Gly-Thr (free acid) is a high-affinity and selective VPAC2 receptor antagonist .
|
-
- HY-P1278
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-P1278A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-P1276A
-
|
Neurokinin-2 receptor antagonist TFA
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor .
|
-
- HY-P1233
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
-
- HY-P1628
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea .
|
-
- HY-P1442
-
|
|
Adrenergic Receptor
|
Cancer
|
|
AdTx1 is a selective α1A-adrenoceptor antagonist (Ki: 0.35 nM). AdTx1 can be used for research of benign prostatic hyperplasia .
|
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-105183
-
|
|
Peptides
|
Others
|
|
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
|
-
- HY-P0062
-
-
- HY-P1233A
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
ANQ-11125 TFA is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 TFA blocks motilide-induced contractions in vitro in the rabbit .
|
-
- HY-P0062B
-
-
- HY-P4745
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .
|
-
- HY-P1419
-
|
|
Peptides
|
Cardiovascular Disease
|
|
AP 811 is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 displays >20000-fold selectivity for NPR3 over NPR1. AP 811 abolishes ANP-induced pump stimulation .
|
-
- HY-P1419A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation .
|
-
- HY-P5833
-
|
κ-Bgt
|
nAChR
|
Neurological Disease
|
|
κ-Bungarotoxin (κ-Bgt) is a potent, selective, and slowly reversible antagonist of α3β2 neuronal nicotinic acetylcholine receptors with an IC50 of 2.30 nM .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P1162
-
-
- HY-103294
-
|
|
Peptides
|
Others
|
|
R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
|
-
- HY-P0062A
-
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P1473
-
|
Amylin (8-37) (mouse, rat)
|
Amylin Receptor
|
Metabolic Disease
|
|
Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
|
-
- HY-P1277
-
-
- HY-P1103
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P1167
-
-
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-107627
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
|
-
- HY-P2109
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
|
-
- HY-P1335
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
- HY-P1277A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
|
- HY-P3881
-
- HY-P1103A
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
- HY-P1167A
-
- HY-P5010
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R .
|
- HY-P1335A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
- HY-P1393
-
|
|
Amylin Receptor
|
Endocrinology
|
|
AC 187 is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .
|
- HY-P1078
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
|
- HY-P1215
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
- HY-P1215A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
- HY-P6292
-
|
|
Peptides
|
Neurological Disease
|
|
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
|
- HY-A0261
-
|
ICI-50123
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
|
- HY-P2093
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
- HY-P1078A
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
|
- HY-P1209A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
PG106 TFA is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50= 210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor .
|
- HY-P2093B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P2093A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
|
- HY-P1393A
-
|
|
Amylin Receptor
|
Endocrinology
|
|
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .
|
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
- HY-P1209
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
- HY-P0039
-
|
|
Bombesin Receptor
|
Cancer
|
|
BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer .
|
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
- HY-P6292A
-
|
|
Peptides
|
Neurological Disease
|
|
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
|
- HY-101230
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom .
|
- HY-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
- HY-100832
-
UNC3866
2 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
|
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
- HY-P3057
-
- HY-P10427
-
|
|
CXCR
HIV
|
Infection
|
|
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
|
- HY-P1108
-
|
|
CFTR
|
Others
|
|
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
|
- HY-100832A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
|
- HY-108055
-
|
|
Urotensin Receptor
Peptides
|
Cardiovascular Disease
|
|
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
|
- HY-12378
-
BQ-123
2 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
- HY-P1202
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively .
|
- HY-P1202A
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively .
|
- HY-P1216A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
|
- HY-P1263
-
- HY-P1264
-
|
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
|
- HY-P1102
-
TC14012
2 Publications Verification
|
CXCR
HIV
|
Infection
Cancer
|
|
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
|
- HY-P1108A
-
|
|
CFTR
|
Others
|
|
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
|
- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
- HY-P1194
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
|
- HY-P1263A
-
- HY-P1159
-
|
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors .
|
- HY-P1194A
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation .
|
- HY-P1102A
-
|
|
CXCR
HIV
|
Infection
Cancer
|
|
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
|
- HY-P1213A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
|
- HY-P1213
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
|
- HY-P1159A
-
|
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP TFA is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP TFA has no activity on glucagon, secretin or GRF receptors .
|
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
- HY-P2055
-
|
|
Peptides
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
- HY-103277
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
- HY-103277A
-
|
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
|
- HY-P2264
-
|
|
Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
|
- HY-P1130
-
|
Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is a selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits Ki values of 13.1 nM and 420 nM for GalR2 and GalR1, respectively. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain) .
|
- HY-P1320
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
- HY-P1320A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
- HY-P1454
-
Fz7-21
3 Publications Verification
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs the function of FZD7 in Wnt–β-catenin signalling and stem cell function in intestinal organoids .
|
- HY-P1454A
-
|
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA is a potent peptide antagonist of FZD7 receptors , selectively binds to FZD7 CRD subclass and alters the conformation of the CRD and the architecture of its lipid-binding groove. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 TFA impairs the function of FZD7 in Wnt-β-catenin signalling and stem cell function in intestinal organoids .
|
- HY-P1106
-
|
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study .
|
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
- HY-P1106A
-
|
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study .
|
- HY-P10429
-
|
|
CXCR
|
Infection
|
|
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
|
- HY-P2446
-
|
APTAA-LHRH
|
Peptides
|
Endocrinology
|
|
ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.
|
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a selective D1-D2 heterogeneous antagonist. TAT-D1 peptide destroys the heterodimer of the D1-D2 receptor by interacting with the specific domain of the D2 receptor through its unique amino acid sequence, in particular the two glutamate residues at the C terminal of the D1 receptor. TAT-D1 peptide can be used to study the role of D1-D2 receptor heterodimers in the regulation of depressive and anxiety-like behaviors .
|
- HY-P1110
-
AF12198
1 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990061
-
|
JTX 8064
|
Inhibitory Antibodies
|
Inflammation/Immunology
Cancer
|
|
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor .
|
-
- HY-P99483
-
|
AT 004; VT 007
|
CD20
Adenosine Receptor
|
Cancer
|
|
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .
|
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-16346S
-
|
|
|
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
|
-
-
- HY-B0298AS
-
1 Publications Verification
|
|
Clemastine-d5 (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
|
-
-
- HY-14447S
-
|
|
|
Bilastine-d6 is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria[1][2].
|
-
-
- HY-22437S
-
|
|
|
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
|
-
-
- HY-22437S1
-
|
|
|
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
|
-
-
- HY-17037S
-
|
|
|
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
|
-
-
- HY-76511S
-
|
|
|
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
|
-
-
- HY-16582AS
-
|
|
|
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
|
-
-
- HY-16578S
-
|
|
|
GW9662-d5 is the deuterium labeled GW9662. GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively[1][2].
|
-
-
- HY-17497S
-
|
|
|
Acebutolol-d7 is a deuterium labeled Acebutolol. Acebutolol is a selective β1 adrenergic receptor antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias[1].
|
-
-
- HY-159578S
-
|
|
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
-
- HY-17000S
-
|
|
|
Tolvaptan-d7 is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].
|
-
-
- HY-A0033S1
-
|
|
|
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
|
-
-
- HY-13004S
-
|
|
|
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
|
-
-
- HY-119802S
-
|
|
|
Practolol-d7 is the deuterium labeled Practolol. Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias[1][2][3].
|
-
-
- HY-10888S
-
|
|
|
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
|
-
-
- HY-13209S
-
|
|
|
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
|
-
-
- HY-B0532S
-
|
|
|
Trifluoperazine-d8 is a deuterium labeled Trifluoperazine. Trifluoperazine is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor [1][2].
|
-
-
- HY-17503AS
-
|
|
|
Metoprolol-d7 (hydrochloride) is the deuterium labeled Metoprolol. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3][4].
|
-
-
- HY-B0745S
-
|
|
|
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
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- HY-17503S3
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Metoprolol-d5 is the deuterium labeled Metoprolol[1]. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[2][3][4].
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- HY-19532S
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ZM241385-d7 is a deuterated form of ZM241385 (HY-19532). ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM .
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- HY-17503BS
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Metoprolol-d6 (tartrate) is the deuterium labeled Metoprolol tartrate. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3][4].
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- HY-B0411S
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Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
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- HY-14136S
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Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
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- HY-B0321S
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Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
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- HY-13738S
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Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
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- HY-13955S1
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Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
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- HY-13955S
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Telmisartan-d3 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
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- HY-13738S2
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Raloxifene-d4 (hydrochloride) is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
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- HY-13738S3
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Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
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- HY-B0462AS
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Azelastine- 13C,d3 is deuterium labeled Azelastine. Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
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- HY-14940S
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Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].
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- HY-14137S
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Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
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- HY-15731S
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Estetrol-d4 is the deuterium labeled Estetrol. Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast[1][2].
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- HY-13955S2
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Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
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- HY-111372S
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Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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- HY-B0539S
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Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B0725S
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Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
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- HY-B0539S1
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Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B0539S3
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Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B0251S
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Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
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- HY-13738S4
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Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
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- HY-13315S1
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Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
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- HY-13315S
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Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
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- HY-13955S3
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Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
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- HY-B0539S4
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Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
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- HY-B0281AS
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Ranitidine-d6 (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].
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- HY-B0309S2
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Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
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- HY-10053S1
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Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
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- HY-14153AS
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Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
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- HY-B0309S1
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Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
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- HY-117743S
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Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
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- HY-B0539S2
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Desloratadine-3,3,5,5-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B1396S
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Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
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- HY-108411S
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Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
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- HY-B0640S
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Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
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- HY-B1396S1
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Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
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- HY-B0192S
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Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
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- HY-B0233S1
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Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
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- HY-W062109S
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Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
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- HY-B0233S2
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Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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- HY-10046S
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Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
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- HY-B0702S
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Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
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- HY-132670S
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(R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
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- HY-B0233S
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Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].
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- HY-14914S1
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Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].
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- HY-10119S
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Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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- HY-117743S1
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Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
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- HY-18346S
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Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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- HY-B0462S
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Azelastine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Azelastine hydrochloride. Azelastine- 13C,d3 (hydrochloride), an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine- 13C,d3 (hydrochloride) can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
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- HY-107322S
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Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
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- HY-B0290S1
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Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
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- HY-A0030S
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Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
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- HY-17037S1
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Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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- HY-B0391S1
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Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
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- HY-107322AS1
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Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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- HY-76569S1
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(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-B0203BS2
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(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
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- HY-B0135S
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Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].
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- HY-10564S
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Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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- HY-17038S1
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Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
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- HY-17038S2
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Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
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- HY-B0822S1
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Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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- HY-14541S2
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Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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Product Name |
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Classification |
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- HY-151391
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Alkynes
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LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-155481A
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Azide
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CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM .
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- HY-159578S
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Azide
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VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
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- HY-159584
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Azide
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LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
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Product Name |
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Classification |
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- HY-148695B
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Aptamers
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ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
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- HY-148695C
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Aptamers
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ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
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