Search Result
Results for "
selective agonist
" in MedChemExpress (MCE) Product Catalog:
1531
Inhibitors & Agonists
4
Biochemical Assay Reagents
87
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-107327
-
|
(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
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-156532C
-
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5-HT Receptor
|
Neurological Disease
|
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(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values ??for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .
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-
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- HY-103549
-
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mGluR
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Neurological Disease
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Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .
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-
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- HY-162618
-
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Cannabinoid Receptor
|
Neurological Disease
|
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PSB-KK1445 is a potent and selective GPR18 agonist with EC50s of 45.4 nM and 124 nM for human and mouse GPR18, respectively. PSB-KK1445 displays >200-fold selectivity versus both CB receptor subtypes, GPR55, and GPR183 .
|
-
-
- HY-107327R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
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-123302
-
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GPR55
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Neurological Disease
|
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CID1172084 (compound 3) is a selective GPR55 agonist (EC50=0.16 μM). CID1172084 is more than 100-fold selective for GPR55 over GPR35, CB1, and CB2. CID1172084 can be used to further explore the biological functions and signaling pathways of the GPR55 receptor .
|
-
-
- HY-151230
-
|
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Estrogen Receptor/ERR
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Cancer
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(-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer .
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-
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- HY-137530
-
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8-Methylamino-cAMP
|
PKA
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Others
|
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8-MA-cAMP (8-Methylamino-cAMP) is a cyclic AMP analog that acts as a site-selective PKA agonist with similar affinity for the B site of type I and type II protein kinase A. 8-MA-cAMP is used in conjunction with priming analogs that show site A preference, such as 8-piperidinyl cAMP, to achieve selective stimulation of type I .
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-
-
- HY-114732
-
|
|
Adrenergic Receptor
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Others
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Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes .
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-
- HY-161511
-
|
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5-HT Receptor
|
Neurological Disease
|
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LPH-5 is a selective 5-HT2A receptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2A receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2A receptor. LPH-5 can be used to further explore the 5-HT2A receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .
|
-
-
- HY-14342
-
MK-5046
2 Publications Verification
|
Bombesin Receptor
|
Metabolic Disease
|
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MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
-
- HY-14342A
-
|
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Others
|
Metabolic Disease
|
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(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
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- HY-156993
-
-
-
- HY-143896
-
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STING
|
Cancer
|
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STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly .
|
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- HY-132217
-
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Cannabinoid Receptor
|
Neurological Disease
|
|
CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2 .
|
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- HY-W095200
-
-
-
- HY-101492
-
-
-
- HY-111358
-
-
-
- HY-110018
-
-
-
- HY-19320
-
-
-
- HY-121091
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-
-
- HY-139177
-
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PPAR
|
Cardiovascular Disease
|
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PPARα agonist 2 (compound 4u) is a potent and selective PPARα agonist with an EC50 of 37 nM. PPARα agonist 2 exhibits >2,700-fold selectivity for PPARα over other PPAR isoforms. PPARα agonist 2 has the potential for retinal disorders research .
|
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- HY-112921A
-
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STING
|
Inflammation/Immunology
|
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diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
|
-
-
- HY-112921B
-
|
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STING
|
Inflammation/Immunology
Cancer
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diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
|
-
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- HY-146141
-
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Ephrin Receptor
|
Cancer
|
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EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB .
|
-
-
- HY-159583
-
-
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- HY-100469
-
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LXR
|
Cardiovascular Disease
|
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LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis .
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- HY-146480
-
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PPAR
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Cancer
|
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PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases .
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-
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- HY-146482
-
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PPAR
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Cancer
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PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases .
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-
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- HY-108936
-
-
-
- HY-111748
-
-
-
- HY-162232A
-
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mGluR
|
Neurological Disease
|
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mGluR2 agonist 1 hydrochloride is a potent selective agonist for metabotropic glutamate receptors mGluR 2 with EC50 of 82 nM .
|
-
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- HY-116468
-
-
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- HY-148198
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-
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- HY-155307
-
-
-
- HY-155306
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-
-
- HY-19673
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-
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- HY-112921
-
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STING
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Inflammation/Immunology
|
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diABZI STING agonist-1 tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
|
-
-
- 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 .
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-
-
- HY-103039
-
-
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- HY-162827
-
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RAR/RXR
Apoptosis
|
Cancer
|
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RAR/RXR agonist-1 (compound 7) is a chlorinated retinoic acid isomer, a selective RARα agonist and a partial RXRα agonist. RAR/RXR agonist-1 can activate RXRα and induce G2/M arrest and apoptosis in cancer cells .
|
-
-
- HY-135982
-
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GPR109A
|
Metabolic Disease
|
|
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a .
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- HY-17354
-
-
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- HY-14917
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-
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- HY-P1013
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-
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- HY-14864
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-
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- HY-14864A
-
-
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- HY-19998
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-
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- HY-17618
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-
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- HY-101039A
-
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Opioid Receptor
|
Neurological Disease
|
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AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
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- HY-139847
-
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ROR
|
Inflammation/Immunology
|
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RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
|
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- HY-101039
-
-
- HY-19945
-
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GABA Receptor
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Neurological Disease
|
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DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
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- HY-107580
-
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GPR109A
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Cardiovascular Disease
Metabolic Disease
|
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GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptor GPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases .
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- HY-P2518
-
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Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
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Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
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- HY-108711
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-
- HY-138695
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- HY-U00038
-
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ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate
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mAChR
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Neurological Disease
|
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ENS-163 phosphate is a selective muscarinic M1 receptor agonist.
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- HY-13201
-
-
- HY-13201A
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- HY-17354A
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Arbaclofen hydrochloride; STX 209 hydrochloride
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GABA Receptor
|
Neurological Disease
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(R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist .
|
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- HY-U00216
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-
- HY-33353
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-
- HY-103704
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-
- HY-100532
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-
- HY-156992
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- HY-146438
-
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PPAR
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Cancer
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PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
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- HY-P1123
-
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ATP Citrate Lyase
Free Fatty Acid Receptor
|
Metabolic Disease
|
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MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120 .
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- HY-122737
-
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ROR
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Inflammation/Immunology
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RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD .
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- HY-P2518A
-
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Protease Activated Receptor (PAR)
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Cancer
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Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
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- HY-146439
-
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PPAR
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Cancer
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PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
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- HY-103418
-
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Dopamine Receptor
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Neurological Disease
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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) .
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- HY-162786
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- HY-146275
-
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LXR
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Cancer
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LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma .
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- HY-150186
-
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RXFP Receptor
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Metabolic Disease
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RXFP2 agonist 2 is a selective，orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis .
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- HY-147501
-
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Thyroid Hormone Receptor
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Metabolic Disease
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TRβ agonist 3 (Compound 3) is a potent agonist of TRβ. TRβ agonist 3 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 3 is a new potential TRβ-selective thyromimetics .
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- HY-147500
-
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Thyroid Hormone Receptor
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Metabolic Disease
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TRβ agonist 2 (Compound 1) is a potent agonist of TRβ. TRβ agonist 2 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 2 is a new potential TRβ-selective thyromimetics .
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- HY-B0374A
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-
- HY-101274
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-
- HY-17622
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-
- HY-101973
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- HY-19661
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-
- HY-P1336
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-
- HY-111068
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- HY-21098A
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- HY-100273
-
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RAR/RXR
Autophagy
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Cancer
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AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
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- HY-107399
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-
- HY-P1013A
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- HY-12236A
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- HY-157294
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- HY-B0197S
-
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GR-85548A-d3-1
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5-HT Receptor
|
Neurological Disease
|
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Naratriptan-d3 is the deuterium labeled Naratriptan[1]. Naratriptan is a selective 5-HT1 receptor subtype agonist[2].
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- HY-153265
-
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Others
|
Metabolic Disease
|
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TAS2R14 agonist-2 (compound 28.1) is a potent and selective TAS2R14 inhibitor with an EC50 value of 72 nM .
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- HY-153912
-
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5-HT Receptor
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Others
|
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5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor .
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- HY-147511
-
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PPAR
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Others
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PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM) .
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- HY-103665
-
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STING
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Cancer
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STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer .
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- HY-103665A
-
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STING
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Cancer
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STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer .
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- HY-141454
-
-
- HY-141454A
-
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Toll-like Receptor (TLR)
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Inflammation/Immunology
|
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TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM) .
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- HY-143271
-
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ROR
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Inflammation/Immunology
|
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RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC50: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis .
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- HY-162232
-
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mGluR
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Neurological Disease
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mGluR2 agonist 1 (Compound 5b) is a potent and selective metabotropic glutamate 2 receptor (mGluR) agonist with an EC50 of 82 nM. mGluR2 agonist 1 can be used for the research of central nervous system (CNS) diseases .
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- HY-114411
-
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Estrogen Receptor/ERR
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Cancer
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ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC50 of 40 nM .
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- HY-115764
-
-
- HY-147351
-
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- HY-156532
-
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5-HT Receptor
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Neurological Disease
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5-HT2C agonist-3 ((+)-19) is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 has antipsychotic drug-like activity. 5-HT2C agonist-3 blocks Amphetamine-induced hyperactivity .
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- HY-160021
-
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ROR
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Inflammation/Immunology
|
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RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
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- HY-101582
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-
- HY-79593
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-
- HY-107216
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-
- HY-19468
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-
- HY-11077
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-
- HY-100327
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- HY-120973A
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-
- HY-12236
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-
- HY-N3891
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-
- HY-12375
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-
- HY-21098
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- HY-147637
-
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Ephrin Receptor
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Cancer
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EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation .
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- HY-100837
-
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iGluR
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Neurological Disease
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5-Iodowillardiine is a potent and selective kainate receptor agonist. 5-Iodowillardiine is selective for kainate receptors composed of hGluR5 subunits .
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- HY-126293
-
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Apelin Receptor (APJ)
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Cardiovascular Disease
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Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0 .
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- HY-B0010S
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-
- HY-132195
-
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ROR
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Inflammation/Immunology
|
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RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis .
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- HY-10475
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CD336; NSC608001; Ro 40-6055
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RAR/RXR
Autophagy
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Cancer
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AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
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- HY-P0226
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- HY-101384A
-
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Dopamine Receptor
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Others
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Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
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- HY-N6629
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-
- HY-100291
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-
- HY-107319
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-
- HY-109032
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DS-8500a
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GPR119
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Metabolic Disease
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Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
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- HY-107395
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-
- HY-143227
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-
- HY-125382
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-
- HY-P1011
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- HY-156532A
-
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5-HT Receptor
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Neurological Disease
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5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 free base has antipsychotic drug-like activity. 5-HT2C agonist-3 free base blocks Amphetamine-induced hyperactivity .
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- HY-150028
-
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Cannabinoid Receptor
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Inflammation/Immunology
|
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CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
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- HY-14773S
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-
- HY-131338
-
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ROR
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Inflammation/Immunology
|
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RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC50 of 63.8 nM .
|
-
- HY-144126
-
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LPL Receptor
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Inflammation/Immunology
|
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S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
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- HY-149833
-
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Estrogen Receptor/ERR
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Infection
Metabolic Disease
|
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ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities .
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- HY-162162
-
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RAR/RXR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
RXR agonist 1 (Compound 33) is a highly selective RXR agonist, with EC50s of 9 nM, 18 nM, and 11 nM for RXRα, RXRβ, and RXRγ, respectively. RXR agonist 1 binds to RXR with high affinity (Kd = 0.03 μM) .
|
-
- HY-103170
-
|
|
Adenosine Receptor
|
Others
|
|
LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively .
|
-
- HY-12761
-
-
- HY-146997
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of 21 nM. TRβ agonist 1 can be used for researching dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH) .
|
-
- HY-10013
-
|
MK-0364
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
|
-
- HY-13239
-
|
|
mGluR
|
Neurological Disease
|
|
LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
|
-
- HY-10480
-
-
- HY-14773
-
-
- HY-16086
-
|
DRF 2593; NN 2344
|
PPAR
|
Metabolic Disease
|
|
Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
|
-
- HY-B0374
-
-
- HY-13421
-
-
- HY-101271
-
-
- HY-16465
-
-
- HY-P1480
-
-
- HY-14785
-
-
- HY-P0226A
-
-
- HY-14785A
-
|
NLX-112 hydrochloride; F 13640 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT1A receptor agonist.
|
-
- HY-103098
-
-
- HY-P1738
-
-
![[Sar9] Substance P](//file.medchemexpress.eu/product_pic/hy-p1738.gif)
- HY-P1334
-
-
- HY-138809
-
-
- HY-135259
-
-
- HY-P2572
-
-
- HY-141494
-
|
|
PPAR
|
Metabolic Disease
|
|
Pparδ agonist 5, an orally active PPARδ-selective agonist (EC50=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo .
|
-
- HY-139702
-
|
|
Integrin
|
Cancer
|
|
α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
|
-
- HY-160031
-
|
|
GLP Receptor
|
Cardiovascular Disease
|
|
GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
|
-
- HY-159582
-
|
|
Others
|
Cardiovascular Disease
|
|
ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC50=69 nM, Emax=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis .
|
-
- HY-152576
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
|
-
- HY-50911
-
|
FXR-450; XL335; WAY-362450
|
FXR
Autophagy
|
Metabolic Disease
Cancer
|
|
Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM .
|
-
- HY-15291
-
|
|
GPR119
|
Metabolic Disease
|
|
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
|
-
- HY-18939
-
-
- HY-12520A
-
|
(±)-SKF-38393 hydrochloride; SKF-38393A
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF 38393 hydrochloride is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM .
|
-
- HY-B0769
-
-
- HY-101386
-
-
- HY-N2371
-
-
- HY-102016
-
-
- HY-103107
-
-
- HY-112627
-
-
- HY-16998
-
|
|
ROR
|
Inflammation/Immunology
|
|
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
|
-
- HY-106094
-
-
- HY-P1334A
-
-
- HY-N2992
-
|
|
RAR/RXR
|
Cancer
|
|
16α-Hydroxytrametenolic acid, a natural triterpene, is a potential retinoid X receptor (RXR) selective agonist .
|
-
- HY-100815A
-
|
L-AMPA
|
iGluR
|
Neurological Disease
|
|
(S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist .
|
-
- HY-108557
-
-
- HY-121415
-
-
- HY-108533
-
|
|
RAR/RXR
|
Cancer
|
|
CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells .
|
-
- HY-148352
-
|
|
PPAR
|
Cancer
|
|
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM .
|
-
- HY-107747
-
-
- HY-156458
-
-
- HY-10658
-
-
- HY-116970
-
-
- HY-108977
-
-
- HY-162491
-
-
- HY-105068
-
-
- HY-123747
-
-
- HY-136623
-
-
- HY-123747A
-
-
- HY-107471
-
|
GP2a
|
Cannabinoid Receptor
|
Cancer
|
|
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells .
|
-
- HY-149803
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity .
|
-
- HY-149804
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity .
|
-
- HY-149803A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity .
|
-
- HY-149804A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
S1R agonist 2 (Compound 8b) hydrochloride is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity .
|
-
- HY-100113
-
-
- HY-162320
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ agonist 12 (compound 9i) is a potent and selective PPARγ agonist with EC50s of 3.98 and 15.42 μM against PPARγ and PPARδ, respectively. PPARγ agonist 12 improves insulin secretion and has anti-diabetic effect .
|
-
- HY-169116
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D5R agonist 1 (Compound 5j) is a selective, orally active and BBB penetrable D5R partial agonist (EC50: 269.7 nM). D5R agonist 1 enhances the cognition in the Scopolamine (HY-N0296)-induced amnesia model .
|
-
- HY-121542
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .
|
-
- HY-14652
-
-
- HY-14413
-
|
ML 176
|
ROR
|
Metabolic Disease
|
|
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM .
|
-
- HY-B0566
-
-
- HY-B0735
-
-
- HY-P1033
-
-
![[Pyr1]-Apelin-13](//file.medchemexpress.eu/product_pic/hy-p1033.gif)
- HY-12584
-
-
- HY-101331
-
-
- HY-114025
-
-
- HY-19673A
-
-
- HY-16465A
-
-
- HY-19942A
-
-
- HY-107555
-
-
- HY-107581
-
|
|
GPR109A
|
Metabolic Disease
|
|
MK-1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist .
|
-
- HY-B0726A
-
|
|
mAChR
|
Neurological Disease
|
|
Pilocarpine is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
|
-
- HY-108698
-
|
(-)-3-PPP hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Preclamol hydrochloride ((-)-3-PPP hydrochloride) is a selective dopamine autoreceptor agonist. Preclamol hydrochloride has the potential for the research of schizophrenia .
|
-
- HY-100843
-
-
- HY-13239A
-
|
|
mGluR
|
Neurological Disease
|
|
LY2979165 free base is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
|
-
- HY-U00391
-
-
- HY-79593S2
-
-
- HY-112217A
-
|
|
nAChR
|
Neurological Disease
|
|
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively .
|
-
- HY-157796
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
|
-
- HY-P10639
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR2 agonist P32 (Ac-RHYPYWR-OH) is a C5aR2-selective agonist. C5aR2 agonist P32 has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo .
|
-
- HY-101609
-
|
E4424
|
5-HT Receptor
|
Neurological Disease
|
|
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
|
-
- HY-12199
-
-
- HY-15601
-
-
- HY-12199B
-
-
- HY-B0197
-
|
GR-85548A
|
5-HT Receptor
|
Neurological Disease
|
|
Naratriptan is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.
|
-
- HY-B0197A
-
|
GR-85548A hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.
|
-
- HY-19774
-
-
- HY-B0189S1
-
-
- HY-128604
-
|
|
ROR
|
Cancer
|
|
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM .
|
-
- HY-103410
-
|
EMD 45609 hydrochloride
|
Dopamine Receptor
|
Cardiovascular Disease
|
|
Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo .
|
-
- HY-103140
-
-
- HY-108528
-
-
- HY-Z9063
-
|
|
Drug Metabolite
|
Others
|
|
1-epi-Regadenoson is an αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .
|
-
- HY-107747A
-
-
- HY-18354
-
|
|
GPR119
|
Metabolic Disease
|
|
GSK1104252A is a potent and selective GPR119 agonist. GSK1104252A can be used for type 2 diabetes research .
|
-
- HY-117926
-
|
|
RAR/RXR
|
Cancer
|
|
AGN 191701 is a selective retinoic acid X receptor (RXR) agonist that causes liver enlargement in rats without hepatocellular necrosis .
|
-
- HY-105112
-
-
- HY-129648
-
-
- HY-P2018
-
-
- HY-109527
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
|
-
- HY-149218
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research .
|
-
- HY-111406
-
|
DE-117
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering agent.
|
-
- HY-P3876
-
-
- HY-103246
-
|
|
Androgen Receptor
|
Cancer
|
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist .
|
-
- HY-119943B
-
|
|
Others
|
Neurological Disease
|
|
(R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .
|
-
- HY-109064
-
|
Oxycodegol; NKTR-181
|
Opioid Receptor
|
Neurological Disease
|
|
Loxicodegol (Oxycodegol) is a first-in-class, long-acting, orally active, and selective mu-opioid agonist with structural properties that reduce its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists .
|
-
- HY-150029
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively .
|
-
- HY-14831
-
|
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
- HY-12199A
-
-
- HY-B0197AS
-
-
- HY-14426
-
-
- HY-101419
-
-
- HY-107675
-
|
Deformylflustrabromine hydrochloride; dFBr hydrochloride
|
nAChR
|
Neurological Disease
|
|
Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
|
-
- HY-P1588
-
-
- HY-P0210
-
DAMGO
4 Publications Verification
|
Opioid Receptor
|
Cancer
|
|
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-15401
-
|
|
5-HT Receptor
|
Cancer
|
|
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5±1.1 nM.
|
-
- HY-P0177
-
-
- HY-14351
-
-
- HY-115765
-
-
- HY-101049
-
-
- HY-B1481B
-
|
Isoetarine hydrochloride
|
Others
|
Infection
|
|
Isoetharine hydrochloride is selective, short-acting and orally active β-agonist which is widely used as a bronchodilator in the research of inhalation research .
|
-
- HY-P3870
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
|
-
- HY-P3870A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
|
-
- HY-148846
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Mosapride N-Oxide is a major active metabolite of Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
|
-
- HY-120633A
-
-
- HY-161105
-
|
|
5-HT Receptor
|
Others
|
|
FPIP is a selectivity agonist of 5-HT1A with a functional potency (pEC50=8.92) .
|
-
- HY-19206
-
-
- HY-124208
-
-
- HY-B0007B
-
|
|
GABA Receptor
|
Neurological Disease
|
|
(S)-Baclofen is a selective GABAB receptor agonist with the IC50 values of 1.77 μM and 1564 μM for GABAB and GABAA, respectively .
|
-
- HY-124208A
-
-
- HY-103446
-
-
- HY-P1198
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
|
-
- HY-19434A
-
|
|
iGluR
mGluR
|
Neurological Disease
|
|
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively .
|
-
- HY-115766
-
|
|
nAChR
|
Neurological Disease
|
|
Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
|
-
- HY-158194
-
|
|
Adrenergic Receptor
|
Cancer
|
|
α2C adrenoceptor agonist 1 (Compound A) is an orally active, highly selective, and non-central nervous system penetrating agonist for the α2C-adrenoceptor, with EC50 and Ki values of 108 nM and 12 nM, respectively. α2C adrenoceptor agonist 1 can be used in the study of nasal congestion .
|
-
- HY-19863
-
-
- HY-B0545
-
-
- HY-17584
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-18687
-
-
- HY-12216
-
-
- HY-101192
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
|
-
- HY-P1012
-
-
![[Sar9,Met(O2)11]-Substance P](//file.medchemexpress.eu/product_pic/hy-p1012.gif)
- HY-111200
-
-
- HY-108526
-
|
|
RAR/RXR
Autophagy
|
Others
|
|
AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
|
-
- HY-111269
-
-
- HY-P0210B
-
|
|
Opioid Receptor
|
Cancer
|
|
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-111098
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3 .
|
-
- HY-19134
-
-
- HY-12237
-
|
(±)-SKF-38393 hydrobromide
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF 38393 ((±)-SKF-38393) hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM .
|
-
- HY-115763
-
|
3-APPA; CGP 27492; CGA 147823
|
GABA Receptor
|
Neurological Disease
|
|
3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective GABAB receptor agonist .
|
-
- HY-103325
-
-
- HY-103108
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect .
|
-
- HY-101205
-
-
- HY-116622
-
-
- HY-105239A
-
|
FE 202158 acetate
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Selepressin (FE 202158) acetate is a selective vasopressin V1A receptor agonist. Selepressin acetate is a potent vasopressin. Selepressin acetate can be used in the study of septic shock.
|
-
- HY-149584
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
CIDD-0149897 is a potent, selective and brain-penetrant ERβ agonist. CIDD-0149897 exert antitumor functions in glioblastoma .
|
-
- HY-119605
-
|
|
Others
|
Neurological Disease
|
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
|
-
- HY-100915
-
|
CGP 35024
|
GABA Receptor
|
Neurological Disease
|
|
SKF 97541 (CGP 35024) is a potent and selective GABAB agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity .
|
-
- HY-156988
-
-
- HY-162117
-
|
|
mGluR
|
Neurological Disease
|
|
LBG30300 is a subtype-selective mGlu2 receptor agonist EC50 0.6 nM. LBG30300 is blood-brain barrier permeable .
|
-
- HY-N6807S
-
-
- HY-106180
-
|
GR 56072; RG 14202; Selodenoson
|
Adenosine Receptor
|
Neurological Disease
|
|
DTI 0009 is a selective adenosine A1 receptor agonist used to reduce heart rate in patients with atrial fibrillation and to treat arrhythmias .
|
-
- HY-17618R
-
|
|
PPAR
|
Inflammation/Immunology
|
|
Pemafibrate (Standard) is the analytical standard of Pemafibrate. This product is intended for research and analytical applications. Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.
|
-
- HY-17584A
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide acetate is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-162617
-
-
- HY-121740
-
-
- HY-19863A
-
-
- HY-128573
-
|
|
ROR
|
Neurological Disease
|
|
RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively .
|
-
- HY-138953
-
|
|
nAChR
|
Neurological Disease
|
|
Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
|
-
- HY-138953A
-
|
|
nAChR
|
Neurological Disease
|
|
Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
|
-
- HY-116222
-
|
|
Others
|
Endocrinology
|
|
A 53693 is a rigid catecholamine with selective adrenergic agonist activity. A 53693 has affinity for certain rat alpha-2 receptor subtypes. A 53693 shows high selectivity for alpha-2 receptors and, in contrast, has low affinity for alpha-1 receptors. A 53693 is used as a probe in biological studies to explore the molecular interactions of alpha agonist compounds .
|
-
- HY-16684
-
|
IRX-5183; VTP-195183; NRX-195183
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
|
-
- HY-101320A
-
|
ICI-D 7114 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes .
|
-
- HY-116507
-
|
|
nAChR
|
Neurological Disease
|
|
AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
|
-
- HY-101320
-
|
ICI-D 7114
|
Adrenergic Receptor
|
Endocrinology
|
|
ZD-7114 is a potent and selective agonist of β3-adrenergic. ZD-7114 is a selective thermogenic agent in vivo. ZD-7114 can be used in study obesity and diabetes .
|
-
- HY-144111
-
|
|
PPAR
|
Inflammation/Immunology
|
|
PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis .
|
-
- HY-161539
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
|
-
- HY-14601
-
|
U 72107A; AD 4833
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
|
-
- HY-14557
-
-
- HY-13773
-
|
VTX-2337; VTX-378
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
|
-
- HY-19946
-
|
F 11440
|
5-HT Receptor
|
Neurological Disease
|
|
Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
|
-
- HY-P0298
-
-
![[Des-Arg9]-Bradykinin](//file.medchemexpress.eu/product_pic/hy-p0298.gif)
- HY-P0298A
-
-
![[Des-Arg9]-Bradykinin acetate](//file.medchemexpress.eu/product_pic/hy-p0298a.gif)
- HY-14898
-
-
- HY-101787
-
TP-024
1 Publications Verification
FTBMT
|
GPR52
|
Neurological Disease
|
|
TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM . TP-024 has antipsychotic and procognitive properties .
|
-
- HY-P1012A
-
-
![[Sar9,Met(O2)11]-Substance P TFA](//file.medchemexpress.eu/product_pic/hy-p1012a.gif)
- HY-101869
-
|
MRK-409
|
GABA Receptor
|
Neurological Disease
|
|
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
|
-
- HY-Z9064
-
|
|
Others
|
Others
|
|
1-epi-Regadenoson ethyl ester is an intermediate in the synthesis of αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .
|
-
- HY-Z9065
-
|
|
Others
|
Others
|
|
1-epi-Regadenoson hydrazone is an intermediate in the synthesis of αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .
|
-
- HY-P2475
-
-
![[Pro9]-Substance P](//file.medchemexpress.eu/product_pic/hy-p2475.gif)
- HY-136474
-
|
(±)-Amidephrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Amidephrine is a selective agonist of alpha 1-adrenoceptor. Amidephrine inhibits inhibits monopulse field contraction of the vas deferens epithelium and prostate gland .
|
-
- HY-P3870B
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
|
-
- HY-103417
-
-
- HY-111116
-
-
- HY-155437
-
|
|
RAR/RXR
|
Others
|
|
NEt-iFQ is a fluorescent retinoid X receptor (RXR) agonist with potent solvatochromic properties. NEt-iFQ selectively binds to RXR-LBP and fluoresces .
|
-
- HY-W702027
-
|
AL842
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Deterenol hydrochloride (AL842) is a selective beta-agonist. Deterenol hydrochloride causes vasodepressor, anxiety, increasing heart rate, hypotension palpitation and respiratory distress .
|
-
- HY-100704A
-
-
- HY-120004
-
|
|
mAChR
|
Infection
|
|
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
|
-
- HY-110160
-
|
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
|
-
- HY-13788
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent .
|
-
- HY-P0078
-
TRAP-6
4 Publications Verification
PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4 .
|
-
- HY-13788B
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent .
|
-
- HY-P1198A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
|
-
- HY-142441
-
|
|
Others
|
Endocrinology
|
|
THR-β Agonist 1 is a potent and selective agonist of THRβ. Thyroid hormone receptor mediates the physiological activity of thyroid hormones which plays a key role in normal growth and development of the body and in maintaining metabolic balance. THR-β Agonist 1 has the potential for the research of thyroid hormone receptor-related diseases (extracted from patent WO2021104288A1, compound 2) .
|
-
- HY-148115
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders .
|
-
- HY-101640
-
-
- HY-14167
-
-
- HY-111110
-
-
- HY-118930
-
-
- 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-101907
-
ASP7663
1 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions .
|
-
- HY-B1478
-
|
|
Histamine Receptor
NO Synthase
|
Endocrinology
|
|
Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion .
|
-
- HY-116169
-
-
- HY-110047
-
-
- HY-118115
-
|
|
Others
|
Others
|
|
Pyrabactin is a seed-selective abscisic acid (ABA) agonist that acts through Pyrabactin Resistance 1 (PYR1). Pyrabactin is used as a synthetic plant growth inhibitor .
|
-
- HY-100532S
-
-
- HY-101765
-
-
- HY-117059
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has the potential for parkinson research .
|
-
- HY-118930A
-
-
- HY-162660
-
|
|
GPR88
|
Neurological Disease
|
|
BI-9508 is a selective and cross the blood-brain barrier GPR88 agonist. BI-9508 has the potential for the research of neurological disorders .
|
-
- HY-157294A
-
|
|
Glucocorticoid Receptor
|
Cancer
|
|
(R)-GSK866 is the (R)-enantiomer of GSK866 (HY-157294). GSK866 is a selective agonist for glucocorticoid receptor with an IC50 of 4.6 nM .
|
-
- HY-123203
-
-
- HY-105315
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AFP-07 is a derivative of 7, 7-difluoroprostacyclic and is a highly potent and selective prostacyclin receptor IP receptor agonist with a Ki value of 0.561 nM .
|
-
- HY-126593
-
|
|
Others
|
Others
|
|
Cryosim-3 is a TRPM8 receptor agonist with activity in selectively activating TRPM8, increasing tear secretion in animal models, and relieving ocular discomfort.
|
-
- HY-154829A
-
|
|
Others
|
Inflammation/Immunology
|
|
AC-099 hydrochloride (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 hydrochloride attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- HY-154829
-
|
|
Others
|
Inflammation/Immunology
|
|
AC-099 (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- 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-14442
-
-
- HY-162579
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC50 value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7, thereby inducing the secretion of TLR7-regulated cytokines IL-12, TNF-αand IFN-αin human PBMC cells. TLR7 agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents .
|
-
- HY-103229
-
|
|
iGluR
|
Neurological Disease
|
|
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
|
-
- HY-N2333
-
|
(+)-Resiniferatoxin
|
TRP Channel
|
Cardiovascular Disease
|
|
Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period .
|
-
- HY-111455
-
LP-211
1 Publications Verification
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-101310
-
|
|
iGluR
|
Neurological Disease
|
|
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively .
|
-
- HY-106278
-
|
|
PPAR
|
Metabolic Disease
|
|
GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia .
|
-
- HY-149702
-
|
|
mAChR
|
Neurological Disease
|
|
M1/M4 muscarinic agonist 1 (compound 41) is a selective muscarinic M4/M1 agonist with EC50 values of 14 and 55 nM for M4 and M1, respectively. M1/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusional disorder, etc .
|
-
- HY-100881
-
-
- HY-N0377
-
-
- HY-U00373
-
-
- HY-109136
-
|
BAY 1101042
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists .
|
-
- HY-P1314
-
-
- HY-B0383A
-
-
- HY-136232
-
|
|
Others
|
Neurological Disease
|
|
PSEM 308 hydrochloride is a pharmacologically selective actuator module (PSAM) agonist. PSEM 308 Activates PSAML141F-GlyR chimeric ion channels .
|
-
- HY-P1030
-
|
|
Neurokinin Receptor
|
Endocrinology
|
|
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
|
-
- HY-108532
-
|
|
RAR/RXR
|
Cancer
|
|
AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0 .
|
-
- HY-138639
-
|
|
GPR52
|
Neurological Disease
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior .
|
-
- HY-110014
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception .
|
-
- HY-108498
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
|
-
- HY-105239
-
|
FE 202158
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Selepressin (FE 202158) is a selective vasopressin V1A receptor agonist. Selepressin is a potent vasopressor. Selepressin can be used in the research of septic shock .
|
-
- HY-P3851
-
-
- HY-122338
-
|
|
FXR
|
Metabolic Disease
|
|
Fexarine is a potent, non-steroidal and selective agonist of farnesoid X receptor (EC50: 38 nM). Fexarine can be used for the research of diseases linked to cholesterol, bile acids .
|
-
- HY-131287
-
|
|
mGluR
|
Neurological Disease
|
|
MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research .
|
-
- HY-121185
-
|
|
Adrenergic Receptor
|
Infection
Inflammation/Immunology
|
|
Hexoprenaline is an orally active and selective β-adrenergic receptor agonist that dilates the bronchi. Hexoprenaline can be used in the study of bronchospasm, including asthma, bronchitis, and emphysema .
|
-
- HY-W335976
-
|
|
5-HT Receptor
|
Cancer
|
|
Almotriptan hydrochloride is a selective agonist of 5-HT 1B/1D Receptor. Almotriptan hydrochloride can used in study of migraine attacks .
|
-
- HY-129293
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AFP-07 free acid is a derivative of 7, 7-difluoroprostacyclic and is a highly potent and selective prostacyclin receptor IP receptor agonist with a Ki value of 0.561 nM .
|
-
- HY-123442
-
-
- HY-101357
-
-
- HY-14856A
-
|
iso-PD 0200390 hydrochloride
|
Others
|
Others
|
|
iso-Atagabalin (iso-PD 0200390) hydrochloride is a stereoisomer of Atagabalin (HY-14856). Atagabalin is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety effect .
|
-
- HY-19690
-
|
KUC-7483 hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Ritobegron, a prodrug of the active compound, KUC-7322, is a selective β3 -adrenoceptor agonist. Ritobegron decreases intravesical pressure with minimal effects on the cardiovascular system.
|
-
- 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 .
|
-
- HY-155184
-
|
|
Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
A3AR agonist 2 (Compound 19) a selective A3AR agonist (Ki: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC50 value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions . A3AR agonist 2 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-12365
-
|
CF-102; 2-Cl-IB-MECA
|
Adenosine Receptor
|
Cancer
|
|
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .
|
-
- HY-108530
-
|
|
RAR/RXR
|
Cancer
|
|
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 .
|
-
- HY-119775
-
|
|
Others
|
Others
|
|
U92016A is a potent and selective agonist of the 5-HT1A receptor, with activities such as high affinity binding to the 5-HT1A receptor in vitro, causing a decrease in body temperature in vivo, and high potency and high intrinsic activity as an agonist in single-cell firing studies.
|
-
- HY-10627A
-
|
|
LXR
|
Cardiovascular Disease
Cancer
|
|
GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively .
|
-
- HY-B1052
-
-
- HY-19770
-
|
|
ROR
|
Inflammation/Immunology
|
|
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding .
|
-
- HY-10013B
-
|
MK0364 (1R,2R)stereoisomer
|
Cannabinoid Receptor
|
Others
|
|
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
|
-
- HY-111343
-
ONC212
3 Publications Verification
|
Apoptosis
|
Endocrinology
Cancer
|
|
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis .
|
-
- HY-107094
-
|
W-212393 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention .
|
-
- HY-B1052A
-
-
- HY-14887
-
|
VA106483
|
Vasopressin Receptor
|
Metabolic Disease
|
|
Fedovapagon (VA106483) is a selective and orally active vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM. Fedovapagon can be used in the research of nocturia .
|
-
- HY-130012
-
-
- HY-P1314A
-
-
- HY-10627
-
|
|
LXR
|
Cardiovascular Disease
|
|
GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively .
|
-
- HY-P1160
-
|
|
GCGR
|
Metabolic Disease
|
|
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes .
|
-
- HY-117196
-
-
- HY-145234
-
-
- HY-107722
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect .
|
-
- HY-148244
-
-
- HY-100938
-
|
1-(3-Chlorophenyl)biguanide hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT3 agonist. m-CPBG hydrochloride can be used for the research of neurological disease .
|
-
- HY-103424
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 dihydrochloride is a selective dopamine D4 receptor agonist. A-412997 dihydrochloride improves cognitive performance in rats and can be used in the research of psychiatric diseases .
|
-
- HY-106851
-
|
FG 10571; PNU 78875
|
GABA Receptor
|
Neurological Disease
|
|
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
|
-
- HY-155099
-
-
- HY-122495
-
|
rel-LY 171555 dihydrochloride; rel-LY 141865 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
rel-Quinpirole (rel-LY 171555) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases .
|
-
- HY-100616A
-
|
trans-1-Aminocyclobutane-1,3-dicarboxylic acid
|
iGluR
|
Neurological Disease
|
|
trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission .
|
-
- HY-W754708
-
|
|
LXR
Na+/K+ ATPase
|
Cardiovascular Disease
|
|
Ouabagenin is a naturally occurring LXR ligand with LXR selective agonist activity. Ouabagenin acts as an EC 3.6.3.9 (Na(+)/K(+)- transport ATPase) inhibitor .
|
-
- HY-120611A
-
-
- HY-12236B
-
-
- HY-111051
-
|
|
nAChR
|
Neurological Disease
|
|
JN403 is an orally active and selective α7 nicotinic acetylcholine receptor agonist. JN403 can be used in the study of central nervous system disorders .
|
-
- HY-124950A
-
|
(+)-GR114297A
|
Others
|
Metabolic Disease
|
|
(+)-Picumeterol is a configurations of Picumeterol (HY-124950). Picumeterol is a potent and selective β2-adrenoceptor agonist with bronchodilator and anti-bronchoconstrictor effects .
|
-
- HY-100704
-
-
- HY-15997B
-
|
(±)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-15997C
-
|
(±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-123376
-
-
- HY-162116
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .
|
-
- HY-B0010B
-
|
(±)Formoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Formoterol ((±)Formoterol) is an orally active β2-selective agonist. Formoterol potently relaxes the peripheral airways through stimulating the beta 2-adrenoceptors selectively as is the case in the central airways and that it significantly inhibits IgE-mediated slow reactive substance of anaphylaxis (SRS-A) release through beta-adrenoceptor stimulation .
|
-
- HY-12023
-
GTx-007
2 Publications Verification
S-4
|
Androgen Receptor
|
Cancer
|
|
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
|
-
- HY-133024
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic .
|
-
- HY-P1341
-
|
Orexin A (17-33) (human, mouse, rat, bovine)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
|
-
- HY-119163
-
-
- HY-14900
-
|
GRC-10693
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
|
-
- HY-122422
-
|
|
5-HT Receptor
|
Others
|
|
Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-103005S
-
|
|
Melatonin Receptor
Drug Metabolite
|
Neurological Disease
Endocrinology
|
|
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
|
-
- HY-P3684A
-
|
|
CRFR
|
Neurological Disease
|
|
[DPro5] Corticotropin Releasing Factor, human, rat TFA is a selective corticotropin releasing factor/hormone R2 (CRH-R2)agonist. [DPro5] Corticotropin Releasing Factor, human, rat TFA fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat .
|
-
![[DPro5] Corticotropin Releasing Factor, human, rat TFA](//file.medchemexpress.eu/product_pic/hy-p3684a.gif)
- HY-120223
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BMS-196085 is an orally active, potent and selective full agonist against human β3 adrenergic receptor with a Ki value of 21 nM. BMS-196085 also has partial agonist activity at the β1 receptor. BMS-196085 is promising for research of obesity and type-II diabetes .
|
-
- HY-162963
-
|
|
PPAR
|
Inflammation/Immunology
|
|
PPARδ agonist 11 (Compound 11) is a selective agonist for PPARδ with an EC50 of 20 nM. PPARδ agonist 11 reduces the levels of nitrite oxide (NO), proinflammatory cytokines TNFα and IL-6 in LPS (HY-D1056)-stimulated RAW264.7 cell, and exhibits anti-inflammatory efficacy via NF-κB pathway. PPARδ agonist 11 exhibits good stability in human liver microsomes and plasma. PPARδ agonist 11 ameliorates Carrageenan (HY-125474)-induced foot edema, and exhibits good pharmacokinetic characteristics with an bioavailability of ca. 100% .
|
-
- HY-138690
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM) .
|
-
- HY-18936
-
-
- HY-P0186
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
|
-
- HY-103207
-
-
- HY-15388S
-
-
- HY-10622
-
-
- HY-120384
-
|
|
ROR
|
Inflammation/Immunology
|
|
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment .
|
-
- HY-101372A
-
|
|
mAChR
|
Neurological Disease
|
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
|
-
- HY-123291
-
-
- HY-100815B
-
|
(±)-AMPA
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors .
|
-
- HY-106147
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system .
|
-
- HY-100815D
-
|
(±)-AMPA monohydrate
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors .
|
-
- HY-132228
-
|
TAK-041; NBI-1065846
|
GPR139
|
Neurological Disease
|
|
Zelatriazin (TAK-041; NBI-1065846) is a potent and selective GPR139 agonist with an EC50 of 22 nM. Zelatriazin has the potential for the research of negative symptoms associated with schizophrenia .
|
-
- HY-123838
-
-
- HY-106432A
-
|
SB-202026 hydrochloride; Memric hydrochloride
|
mAChR
|
Neurological Disease
|
|
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .
|
-
- HY-145128
-
-
- HY-106432
-
|
SB-202026; Memric
|
mAChR
|
Neurological Disease
|
|
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .
|
-
- HY-79593S1
-
-
- HY-103132
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PNU109291 is a potent and selective 5-HT1D agonist. PNU109291 reduces dural plasma extravasation evoked by trigeminal ganglion stimulation .
|
-
- HY-119242
-
-
- HY-14897
-
-
- HY-107667
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 fumarate is a potent and selective neuronal acetylcholine receptor agonist. TC-2559 fumarate is potent and efficacious in the activation of CNS receptors and reduces glutamate-induced neurotoxicity in vitro .
|
-
- HY-10886
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB is used in anxiety disorders research .
|
-
- 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-114550
-
|
|
iGluR
|
Neurological Disease
|
|
LY339434 is a potent and selective agonist for the hydrochloride receptor GluR5. LY339434 affects the rapid death of neurons through n-methyl-D-aspartate (NMDA) receptors .
|
-
- HY-14773R
-
-
- HY-122231
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
MRS3558 is a potent and selective A3AR agonist, with Ki values of 0.6 nM for humans and 0.9 nM for rats, making it suitable for research in the fields of neuropathic pain and anesthesia .
|
-
- HY-105235
-
|
CI-977
|
Opioid Receptor
|
Neurological Disease
|
|
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
|
-
- HY-105235A
-
|
CI-977 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
|
-
- HY-111479
-
-
- HY-131032
-
|
|
Adenosine Receptor
|
Others
|
|
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively .
|
-
- HY-P1341A
-
|
Orexin A (17-33) (human, mouse, rat, bovine) TFA
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
|
-
- HY-162620
-
|
|
Adrenergic Receptor
|
Cancer
|
|
α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
|
-
- HY-163670
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
TLR7 agonist 21 (Compound 27B) is a selective agonist for Toll-like receptor 7(TLR7), with an EC50 of 17.53 nM (for human TLR7) and 41.7 nM (for mouse TLR7). TLR7 agonist 21 stimulates the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, IFN-α1, and IL-4. TLR7 agonist 21 acts as a vaccine adjuvant, increases levels of IgG and IgA, and protects the mouse from influenza virus infections .
|
-
- HY-P5506
-
|
|
Complement System
|
Others
|
|
C5a Receptor agonist, W5Cha (Peptide 1) is a selective complement C5a receptor (C5aR) agonist (EC50=0.2 μM), a hexapeptide derived from the C-terminus of C5a with specific amino acid modifications. C5a Receptor agonist, W5Cha is able to interact with the Arg-206 site of the C5a receptor through its C-terminal arginine, thereby activating the receptor .
|
-
- HY-B1752
-
|
LY 171555; (-)-LY 141865
|
Others
|
Neurological Disease
|
|
Quinpirole (LY 171555) is a dopamine D2/D3 receptor agonist with activity in reducing hypothalamic norepinephrine concentrations. The effects of Quinpirole are not produced by the selective D1 agonist SKF 38393 or the dextrorotatory isomer of Quinpirole, which lacks D2 agonist activity. By activating D2 receptors, Quinpirole leads to a decrease in dopamine metabolites, a decrease in hypothalamic norepinephrine concentrations, and a possible increase in MHPG sulfate by enhancing norepinephrine release .
|
-
- 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-13410
-
|
LY246708 oxalate
|
mAChR
|
Neurological Disease
|
|
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease .
|
-
- HY-16639
-
-
- HY-B0418A
-
|
R-18553 hydrochloride
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-B0584
-
|
Fluprostenol isopropyl ester; AL6221; Flu-Ipr
|
Prostaglandin Receptor
|
Endocrinology
|
|
Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
|
-
- HY-15443
-
-
- HY-B1216
-
-
- 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-107094A
-
|
W-212393
|
Opioid Receptor
|
Neurological Disease
|
|
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention .
|
-
- HY-18295
-
|
LY500307
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities .
|
-
- HY-W013372
-
|
|
Trk Receptor
Apoptosis
|
Neurological Disease
|
|
7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases .
|
-
- HY-105634
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-18760
-
|
|
mGluR
|
Neurological Disease
|
|
LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively) .
|
-
- HY-14304
-
|
MJ 9184
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol (MJ 9184) is a potent and selective β2-adrenoceptor agonist . Zinterol increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM .
|
-
- HY-105170B
-
|
|
nAChR
|
Neurological Disease
|
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease .
|
-
- HY-106147B
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system .
|
-
- HY-P1160A
-
|
|
GCGR
|
Metabolic Disease
|
|
Bay 55-9837 TFA is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 TFA may be a useful therapy for the research of type 2 diabetes .
|
-
- HY-P1752
-
|
|
CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II (human) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior .
|
-
- HY-106007
-
|
INO-8875
|
Adenosine Receptor
|
Inflammation/Immunology
|
Trabodenoson (INO-8875), an adenosine mimetic, is a highly selective Adenosine A1 receptor agonist. Trabodenoson (INO-8875) is used in the study for Primary Open-Angle Glaucoma .
|
-
- HY-134661A
-
CVN424
1 Publications Verification
|
GPR6
|
Neurological Disease
|
|
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research .
|
-
- HY-116459
-
|
AF102A hydrochloride
|
mAChR
|
Neurological Disease
|
|
Trans-Cevimeline (AF102A) (hydrochloride), as a trans-isomer of AF102B, is a M1 selective cholinergic agonist. Trans-Cevimeline (AF102A) (hydrochloride) can be used for the research of Alzheimer's disease .
|
-
- HY-103054
-
|
|
Others
|
Neurological Disease
|
|
RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric research .
|
-
- HY-147220
-
|
Dex-Ox
|
Progesterone Receptor
|
Endocrinology
|
|
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms .
|
-
- HY-114011
-
-
- HY-151264
-
|
|
STING
|
Cancer
|
|
BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer .
|
-
- HY-10480A
-
|
(R)-TAK-875
|
Others
|
Metabolic Disease
|
|
(R)-Fasiglifam is the isomer of Fasiglifam (HY-10480), and can be used as an experimental control. Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
|
-
- HY-129738
-
|
|
Others
|
Cardiovascular Disease
|
|
I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases .
|
-
- HY-160207
-
-
- HY-111006
-
|
UH 232
|
Dopamine Receptor
|
Neurological Disease
|
|
(+)-UH 232 is a partially selective agonist of the D3 receptor with an intrinsic activity of 0.2-0.4. (+)-UH 232 antagonized quinpirole-induced mitogenesis with a Ki value of 9.4 nM .
|
-
- HY-103107A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY334370 hydrochloride is a selective 5-HT1F receptor agonist with a Kd value of 0.446 nM. LY334370 hydrochlorid has anti-migraine activity .
|
-
- HY-120611
-
-
- HY-B0769R
-
-
- HY-163917
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .
|
-
- HY-116480
-
|
|
Others
|
Neurological Disease
|
|
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .
|
-
- HY-100815E
-
|
(±)-AMPA hydrochloride
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) hydrochloride is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
|
-
- HY-105791
-
|
|
Others
|
Inflammation/Immunology
|
|
Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research .
|
-
- HY-13225
-
|
RJR-2403 oxalate; (E)-Metanicotine oxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-13225B
-
|
RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-17416S
-
-
- 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-151811
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
|
-
- HY-126346
-
|
|
GPR84
|
Inflammation/Immunology
|
|
DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .
|
-
- HY-12222
-
|
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
|
-
- HY-10678
-
|
|
PPAR
|
Cardiovascular Disease
|
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-103005
-
-
- HY-P0186A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
|
-
- HY-128770
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor
positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
|
-
- HY-50665
-
|
LY-674
|
PPAR
|
Metabolic Disease
|
|
LY518674 is a potent, selective PPARα agonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis .
|
-
- HY-135392
-
|
AC-279
|
Drug Metabolite
|
Neurological Disease
|
|
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
|
-
- HY-19483
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.
|
-
- 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-P1125
-
4-CMTB
2 Publications Verification
|
Free Fatty Acid Receptor
|
Others
|
|
4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38) .
|
-
- HY-P1752A
-
|
|
CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II, human (TFA) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior .
|
-
- HY-105040C
-
|
LY2140023 hydrochloride
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research .
|
-
- HY-128901
-
|
F 14679 fumarate
|
5-HT Receptor
|
Neurological Disease
|
|
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress .
|
-
- HY-110239
-
|
MP-11
|
mAChR
|
Neurological Disease
|
|
Perlapine is a potent muscarinic DREADD (Designer Receptors Exclusively Activated by Designer agents) agonist Perlapine exhibits >10000-fold selectivity for hM3Dq over hM3 receptors .
|
-
- HY-32345
-
|
BXL-628; Ro-26-9228
|
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells .
|
-
- HY-103536
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galnon is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with Kis of 11.7 and 34.1 μM respectively. Galnon exhibits anticonvulsant and anxiolytic effects .
|
-
- HY-153615
-
|
|
mGluR
|
Neurological Disease
|
|
CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .
|
-
- HY-129271
-
|
Deltorphin A; Dermenkephalin
|
Opioid Receptor
|
Others
|
|
Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
|
-
- HY-100815C
-
|
(±)-AMPA hydrobromide
|
iGluR
|
Neurological Disease
|
|
(RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
|
-
- HY-106949
-
|
|
mAChR
|
Neurological Disease
|
|
Tazomeline is a selective M1 muscarinic receptor agonist. Tazomeline inhibits twitch height in rabbit vas deferens(IC50= 0.001 nM). Tazomeline can be used for research of neuropsychiatric disorders .
|
-
- HY-116586
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
|
-
- 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-158693
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
WLB-87848 is a selective, orally active, and blood-brain barrier (BBB) permeable σ1 receptor agonist with the Ki of 9 nM. WLB-87848 rescues recognition memory impairment .
|
-
- HY-110065
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with a Ki of 6.3 nM. SER-601 has analgesic and antidiabetic properties and can be used for relevant research .
|
-
- HY-B0566R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Guanabenz (Acetate) (Standard) is the analytical standard of Guanabenz (Acetate). This product is intended for research and analytical applications. Guanabenz (Acetate) (BR-750) is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.
|
-
- HY-114700
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
ZINC08438472 is a potent and selective peroxisome proliferator activated receptors-α (PPAR-α) agonist with an EC50 value of 12.1 nM. ZINC08438472 is promising for research of diabetes, hyperlipidaemia and inflammatory disorders .
|
-
- HY-100778
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
SMM-189 is a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research .
|
-
- HY-120949
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-14340
-
|
SAX-187
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM . WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
-
- HY-W746031
-
|
SAX-187 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) hydrochloride is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM . WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
-
- HY-167862
-
|
|
Others
|
Neurological Disease
|
|
UCM-05194 is a selective LPA1 receptor agonist with activity to improve neuropathic pain. UCM-05194 is a LPA1 agonist that exhibits potent and selective properties in its pharmacologically similar properties. UCM-05194 triggers LPA1-mediated cellular effects and leads to internalization of the receptor, resulting in functional inactivation in primary sensory neurons. UCM-05194 effectively reduces pain perception in in vivo models. UCM-05194 can be used to conduct research on progressive systemic diseases .
|
-
- 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-108058A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
|
-
- HY-10680
-
MK-6892
5 Publications Verification
|
GPR109A
|
Cancer
|
|
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
|
-
- HY-100155
-
|
|
Sigma Receptor
|
Cancer
|
|
4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).
|
-
- HY-121885
-
LMD-009
1 Publications Verification
|
CCR
|
Metabolic Disease
Endocrinology
|
|
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM .
|
-
- HY-128064
-
-
- HY-108649A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2768 tetrasodium salt is a moderately potent and selective P2Y2 receptor agonist. MRS2768 tetrasodium salt has a protective effect on cardiomyocytes from ischemic damage in vivo and in vitro .
|
-
- HY-14554
-
|
LY2140023
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research .
|
-
- HY-120160
-
|
CP-86325
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-108038
-
|
|
nAChR
|
Neurological Disease
|
|
ABT-107 is a selective α7 neuronal nicotinic receptor agonist. ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions .
|
-
- HY-118402
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis .
|
-
- HY-129674
-
|
|
nAChR
|
Neurological Disease
|
|
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation .
|
-
- HY-107516
-
|
(S)-3,4-Dicarboxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(S)-3,4-DCPG is a selective agonist of metabotropic glutamate receptor 8a (mGluR8a) with an EC50 of 31 nM in AV12-664 cells expressing human mGluR8 .
|
-
- HY-107741
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys .
|
-
- HY-112071
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease .
|
-
- HY-105155
-
|
RMP 7
|
Bradykinin Receptor
|
Cancer
|
|
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
|
-
- HY-P3877
-
-
- HY-P3891
-
-
- HY-116524
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
|
-
- HY-116046
-
|
|
Melatonin Receptor
|
Others
|
|
GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice .
|
-
- HY-12720B
-
|
ALO 2145 dihydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Apraclonidine (ALO 2145) dihydrochloride, a selective α2 and weak α1 receptor agonist activity, effectively low intraocular pressure (IOP) in eyes. Apraclonidine dihydrochloride is a topical ophthalmic solution .
|
-
- HY-114974
-
-
- HY-B0374R
-
|
|
Imidazoline Receptor
|
Neurological Disease
|
|
Moxonidine (Standard) is the analytical standard of Moxonidine. This product is intended for research and analytical applications. Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
|
-
- HY-139386
-
|
15(S)-Flu-Ipr
|
Others
|
Others
|
|
15β-Travoprost (15(S)-Flu-Ipr) is an enantiomer of Travoprost (HY-B0584). Travoprost, an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist .
|
-
- HY-164463
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
BMI-135 is a selective estrogen mimic, that exhibits agonist activity for estrogen receptor. BMI-135 induces rapid endoplasmic reticulum stress response (UPR) and apoptosis in breast cancer cells .
|
-
- HY-156131
-
|
ADL 2-1294
|
Others
Opioid Receptor
|
Inflammation/Immunology
|
|
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent .
|
-
- HY-14839A
-
-
- HY-110366
-
|
SAX-187 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
-
- HY-P99665
-
|
LY-3209590
|
Insulin Receptor
|
Metabolic Disease
|
|
Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
|
-
- HY-17034A
-
|
(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
- HY-B0061
-
|
SM-3997 citrate
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
|
-
- HY-19838
-
|
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB) .
|
-
- HY-15688
-
|
8-Hydroxy-DPAT hydrobromide
|
5-HT Receptor
|
Neurological Disease
|
|
8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site .
|
-
- HY-12719
-
|
(+)-Medetomidine; (S)-Medetomidine
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
|
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
- HY-14823
-
-
- HY-18941
-
|
LY354740; Eglumetad
|
mGluR
|
Neurological Disease
|
|
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
|
-
- HY-N6868
-
|
dmLSB
|
Sodium Channel
|
Cardiovascular Disease
|
|
Dimethyl lithospermate B (dmLSB) is a selective Na + channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP) .
|
-
- HY-P1279
-
-
![[Lys5,MeLeu9,Nle10]-NKA(4-10)](//file.medchemexpress.eu/product_pic/hy-p1279.gif)
- HY-119943
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease .
|
-
- HY-129527
-
|
|
iGluR
|
Neurological Disease
|
|
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
|
-
- HY-P1167
-
-
![[Orn5]-URP](//file.medchemexpress.eu/product_pic/hy-p1167.gif)
- HY-P2210
-
|
|
GPR171
|
Metabolic Disease
|
|
BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. BigLEN(mouse) can be used to regulate responses associated with food intake and metabolism .
|
-
- HY-116146
-
-
- HY-105124
-
-
- HY-103536A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galnon TFA is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with Kis of 11.7 and 34.1 μM respectively. Galnon TFA exhibits anticonvulsant and anxiolytic effects .
|
-
- HY-117118A
-
-
- HY-126081
-
-
- HY-70081
-
|
PNU-95666E
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole (PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-110131
-
|
|
nAChR
|
Neurological Disease
|
|
A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
|
-
- HY-129103
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
|
-
- HY-118978
-
|
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
PF-00277343 is a selective and skin-penetrable THR-β (Ki: 0.51 nM for THR-β, 8.0 nM for THR-α) agonist. PF-00277343 is effective against androgenetic alopecia in animal models .
|
-
- HY-B0374S1
-
-
- HY-105236
-
|
(Rac)-CI-977 free base
|
Others
|
Neurological Disease
|
|
(Rac)-Enadoline ((Rac)-CI-977 free base) is a selective K-opioid receptor agonist that stereoselectively antagonizes clonic seizures induced by slow intravenous injection of N-methyl-DL-aspartate in mice .
|
-
- HY-W062702
-
|
|
nAChR
|
Neurological Disease
|
|
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia .
|
-
- HY-114853
-
|
|
PPAR
|
Metabolic Disease
|
|
BVT.13 is an orally active and selective PPARγ agonist with a maximal efficacy similar to that of Rosiglitazone (HY-17386). In addition, BVT.13 exhibits antidiabetic activity in ob/ob mice .
|
-
- HY-110003
-
|
ACPA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) .
|
-
- HY-117378A
-
|
KRP-204 hydrochloride
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
N-5984 (KRP-204) hydrochloride is a potent and selective agonist of β3-adrenergic receptor. N-5984 hydrochloride can be used for research of obesity and diabetes mellitus .
|
-
- HY-136258
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
|
-
- 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-147310
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
CU-CPD107 is a potent, selective toll-like receptor 8 (TLR 8) agonist. CU-CPD107 inhibits TLR8 signaling. CU-CPD107 converts to synergistic agonist activities in the presence of ssRNA and induces TLR8 signaling. CU-CPD107 inhibits proinflammatory factor expression and avoids immune responses in the presence of ssRNA .
|
-
- HY-B0072
-
-
- HY-B0154
-
-
- HY-19608
-
-
- HY-108449
-
|
WS-12; AR-15512; AVX-012
|
TRP Channel
|
Cancer
|
|
Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
|
-
- HY-111271
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
|
-
- HY-B0545S
-
|
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
|
|
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
|
-
- HY-122190
-
|
|
mAChR
|
Neurological Disease
|
|
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM .
|
-
- HY-103181
-
|
CPA; UK-80882
|
Adenosine Receptor
|
Neurological Disease
|
|
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively .
|
-
- HY-117071
-
|
Ro 115-1240
|
Adrenergic Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function .
|
-
- HY-109137
-
|
GS-9688
|
Toll-like Receptor (TLR)
HBV
|
Infection
|
|
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection .
|
-
- HY-108472
-
|
7-Allyl-8-oxoguanosine; RWJ 21757
|
Toll-like Receptor (TLR)
Influenza Virus
|
Infection
Cancer
|
|
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist .
|
-
- HY-108661
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
|
-
- HY-109197
-
|
EYP001
|
FXR
HBV
|
Infection
|
|
Vonafexor (EYP001) is an orally active, non-steroidal and selective FXR agonist. Vonafexor shows significant HBsAg reduction when combined with Peg-IFNα. Vonafexor can be used for anti-HBV research .
|
-
- HY-P1279A
-
-
![[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA](//file.medchemexpress.eu/product_pic/hy-p1279a.gif)
- HY-110060
-
|
|
Complement System
|
Inflammation/Immunology
|
|
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases .
|
-
- HY-129098
-
DMHCA
1 Publications Verification
|
LXR
|
Metabolic Disease
|
|
DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects?and can be used for the research of cholesterol homeostasis diabetes .
|
-
- HY-106450
-
|
MRE-0470; WRC 0470
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging .
|
-
- HY-139582
-
|
OC-02
|
nAChR
SARS-CoV
|
Infection
|
|
Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM .
|
-
- HY-101366
-
-
- HY-120160A
-
|
CP 86325 Sodium
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-118339
-
|
|
5-HT Receptor
|
Cancer
|
|
PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension .
|
-
- HY-P3597
-
|
|
CFTR
|
Others
|
|
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with high affinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit .
|
-
- HY-148351
-
|
|
PPAR
|
Cancer
|
|
BAY-0069 is a potent and selective PPARγ inverse agonist with an IC50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer .
|
-
- HY-W580721A
-
|
|
Histamine Receptor
|
Others
|
|
4-Methylhistamine (hydrochloride) is a potent, high affinity H4 receptor agonist Ki of 7 nM. 4-Methylhistamine (hydrochloride) displays more than 100-fold selectivity over other human histamine receptor subtypes .
|
-
- HY-B0545R
-
|
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
Cancer
|
|
Probenecid (Standard) is the analytical standard of Probenecid. This product is intended for research and analytical applications. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
|
-
- HY-P5358
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
|
-
- HY-108661A
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF546 (hydrate) is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 (hydrate) stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
|
-
- 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-162465
-
|
|
STING
|
Infection
Inflammation/Immunology
Cancer
|
|
BDW568 is a STING agonist that can selectively activate the human STING A230 allele. BDW568 can be used to activate STING A230-engineered macrophages in macrophage-based immunotherapy .
|
-
- HY-P10291
-
-
![[Pro34]Neuropeptide Y, porcine](//file.medchemexpress.eu/product_pic/hy-p10291.gif)
- HY-17584R
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide (Standard) is the analytical standard of Linaclotide. This product is intended for research and analytical applications. Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-125284
-
|
SPL7
|
Others
|
Others
|
|
Sphynolactone-7 (SPL7) is an active site-targeting and selective strigolactone receptor (ShHTL7) agonist. Sphynolactone-7 is effective for reducing Striga parasitism without impinging on host strigolactone-related processes .
|
-
- HY-117071A
-
|
Ro 115-1240 hydrochloride
|
Adrenergic Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
Dabuzalgron (Ro 115-1240) hydrochloride is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron hydrochloride protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function .
|
-
- HY-50906
-
|
|
mGluR
|
Neurological Disease
|
|
LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects .
|
-
- HY-P5172
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
|
-
- HY-12365R
-
|
|
Adenosine Receptor
|
Cancer
|
|
Namodenoson (Standard) is the analytical standard of Namodenoson. This product is intended for research and analytical applications. Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .
|
-
- HY-14839
-
-
- HY-15451
-
MDA 19
1 Publications Verification
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-P1295
-
|
Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
|
-
- HY-19775
-
|
|
ROR
|
Inflammation/Immunology
|
|
GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC .
|
-
- HY-112612
-
|
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats .
|
-
- HY-12685
-
|
ONO-4641
|
LPL Receptor
|
Neurological Disease
|
|
Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
|
-
- HY-112612A
-
|
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats .
|
-
- HY-112706
-
|
|
ROR
|
Inflammation/Immunology
|
|
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity .
|
-
- HY-14171S
-
|
LGD1069 d4
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
|
-
- HY-14848
-
|
PRX 00023
|
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K + channel blocker, with IC50 of 3800 nM.
|
-
- HY-P1132
-
-
- HY-116506
-
|
|
RAR/RXR
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .
|
-
- HY-P1167A
-
-
![[Orn5]-URP TFA](//file.medchemexpress.eu/product_pic/hy-p1167a.gif)
- HY-111582
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
BBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of ?59.1?nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .
|
-
- HY-105182
-
|
LY-246708
|
mAChR
|
Neurological Disease
|
|
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
|
-
- HY-110118
-
|
|
PPAR
|
Metabolic Disease
|
|
Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity .
|
-
- HY-18060
-
|
TC-5619
|
nAChR
|
Neurological Disease
|
|
Bradanicline is a highly selective α7 nicotinic acetylcholine receptor (nAChR) agonist (humanα7 nAChR: EC50=17 nM; Ki= 1.4 nM). Bradanicline is used for the research of cognitive disorders .
|
-
- HY-122025
-
|
|
Androgen Receptor
|
Metabolic Disease
|
|
AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
|
-
- HY-119518
-
|
BMS-209641
|
RAR/RXR
|
Cancer
|
|
BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (Kd, 2.5 nM) that is 100 times higher than that for RARα (Kd, 225 nM) or RARγ (Kd, 223 nM) .
|
-
- HY-144397
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases .
|
-
- HY-12720
-
|
ALO 2145 free base
|
Adrenergic Receptor
|
Infection
Neurological Disease
|
|
Apraclonidine (ALO 2145 (free base)), a selective α2 and weak α1 receptor agonist activity, effectively low intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution .
|
-
- HY-P1332
-
|
[D-Ser2, Leu5, Thr6]-enkephalin
|
Opioid Receptor
|
Neurological Disease
|
|
DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor .
|
-
- HY-P1129
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
AR-M1896 is a GalR2 selective agonist with a binding IC50 of 1.76 nM for rat GalR2. AR-M1896 can be used for the research of acute myocardial infarction and neuropathic pain .
|
-
- HY-14601R
-
|
U 72107A (Standard); AD 4833 (Standard)
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (hydrochloride) (Standard) is the analytical standard of Pioglitazone (hydrochloride). This product is intended for research and analytical applications. Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
|
-
- HY-108991
-
|
(-)-T-0509
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
T-0509 ((-)-T-0509) is a selective full agonist of the β1 receptor. T-0509 activates the cAMP signaling pathway through the β1 receptor and enhances myocardial contractility .
|
-
- HY-14557R
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Pimavanserin (Standard) is the analytical standard of Pimavanserin. This product is intended for research and analytical applications. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
|
-
- HY-14848A
-
|
PRX 00023 hydrochloride
|
5-HT Receptor
Potassium Channel
|
Neurological Disease
|
|
Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K + channel blocker, with IC50 of 3800 nM.
|
-
- HY-10626
-
|
|
LXR
FXR
ROR
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
|
-
- HY-P1322
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats .
|
-
![[D-Trp34]-Neuropeptide Y](//file.medchemexpress.eu/product_pic/hy-p1322.gif)
- HY-111509
-
|
|
ROR
|
Inflammation/Immunology
|
|
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) .
|
-
- 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-110092
-
|
|
P2Y Receptor
|
Metabolic Disease
|
|
PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors .
|
-
- HY-117764
-
|
|
mGluR
|
Neurological Disease
|
|
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
|
-
- HY-110092A
-
|
|
P2Y Receptor
|
Cancer
|
|
PSB-1114 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors .
|
-
- HY-122422R
-
|
|
5-HT Receptor
|
Others
|
|
Gepirone (Standard) is the analytical standard of Gepirone. This product is intended for research and analytical applications. Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-10912
-
|
|
FXR
Autophagy
|
Others
|
|
Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .
|
-
- HY-18779
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse .
|
-
- HY-19522A
-
|
MBX-8025 sodium salt; RWJ-800025 sodium salt
|
PPAR
|
Metabolic Disease
|
|
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.
|
-
- HY-100300
-
-
- HY-B0374S
-
|
|
Imidazoline Receptor
|
Neurological Disease
|
|
Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine. Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent[1][2].
|
-
- HY-119486
-
|
PF-06649751; CVL-751
|
Dopamine Receptor
|
Neurological Disease
|
|
Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease .
|
-
- HY-17609
-
|
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-P1132A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect .
|
-
- HY-17642
-
|
UR-7276
|
Prostaglandin Receptor
|
Endocrinology
|
|
Omidenepag (UR-7276), a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2 .
|
-
- HY-103183
-
-
- HY-W014941
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-103101
-
|
|
5-HT Receptor
|
Others
|
|
LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
|
-
- HY-116797
-
|
MS0015203
|
GPR171
|
Metabolic Disease
|
|
MS15203 is a potent and selective GPR171 agonist. MS15203 increases food intake and body weight. MS15203 increases neuronal activity. MS15203 significantly increases the abundance of the mRNAs encoding proSAAS, NPY, AgRP .
|
-
- HY-114794
-
-
- HY-P3462A
-
|
|
CGRP Receptor
|
Metabolic Disease
|
|
Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
|
-
- HY-P3609
-
|
JNJ 38488502; FE 200665
|
Opioid Receptor
|
Neurological Disease
|
|
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
|
-
- HY-100426A
-
|
MKC242
|
5-HT Receptor
|
Neurological Disease
|
|
Osemozotan hydrochloride (MKC242) is a selective 5-HT1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder .
|
-
- 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-120396
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 293284 is a potent and selective 5-HT1A receptor agonist. LY 293284 results in a significant drop in core temperature and consumes more food in cholestasis rat induced by bile duct resection .
|
-
- HY-108499
-
-
- HY-156174
-
|
|
Toll-like Receptor (TLR)
ADC Cytotoxin
|
Cancer
|
|
E104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs .
|
-
- HY-18295A
-
|
rel-LY500307
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
rel-Erteberel is rel isomer of Erteberel (HY-18295). Erteberel is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities .
|
-
- HY-110040
-
-
- HY-13225D
-
|
RJR-2403 fumarate; (E)-Metanicotine fumarate
|
nAChR
|
Neurological Disease
|
|
Rivanicline fumarate is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .
|
-
- HY-P99004
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family .
|
-
- HY-130176
-
|
|
Opioid Receptor
ERK
Adenylate Cyclase
|
Neurological Disease
|
|
UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-107676
-
|
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders .
|
-
- HY-P1390
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors .
|
-
![d[Cha4]-AVP](//file.medchemexpress.eu/product_pic/hy-p1390.gif)
- HY-108497A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Cancer
|
|
L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
|
-
- HY-103105A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
|
-
- HY-W014208
-
|
AF-267B
|
Others
|
Others
|
|
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .
|
-
- HY-P10579
-
|
|
Ephrin Receptor
|
Cancer
|
|
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
|
-
- HY-12184
-
|
|
Others
|
Cardiovascular Disease
|
|
ONO-AE 248 is a selective EP3 receptor agonist with cardioprotective activity. ONO-AE 248 reduces myocardial infarction size by selectively binding to the EP3α receptor in mice. The cardioprotective effect of ONO-AE 248 is independent of hemodynamic effects. The mechanism of ONO-AE 248 may involve activation of protein kinase C and opening of K(ATP) channels .
|
-
- HY-17043
-
-
- HY-15483
-
DY131
3 Publications Verification
GSK 9089
|
Estrogen Receptor/ERR
Smo
|
Endocrinology
Cancer
|
|
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .
|
-
- HY-B0225
-
-
- HY-B0225A
-
|
L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
|
-
- HY-B0471
-
-
- HY-B0225B
-
|
L-(-)-α-Methyldopa hydrate; MK-351 hydrate
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
|
-
- HY-119243
-
|
|
mGluR
|
Neurological Disease
|
|
LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM，EC50=0.47 nM; hmGlu2 Ki=412 nM，EC50=47.5 nM) .
|
-
- HY-103244
-
CITCO
1 Publications Verification
|
Apoptosis
|
Cancer
|
|
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors .
|
-
- HY-123268
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. RO 363 is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility .
|
-
- HY-P1338
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
-
- HY-123268A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility .
|
-
- HY-111253
-
|
|
LPL Receptor
|
Neurological Disease
|
|
CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity .
|
-
- HY-117378
-
|
KRP-204
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus .
|
-
- HY-111292
-
|
|
LPL Receptor
|
Cancer
|
|
CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC50 and EC50 of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases .
|
-
- HY-P4107
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr) .
|
-
- HY-103179
-
|
WAG-994; N6-Cyclohexy-2'-0-methyladenosine
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation .
|
-
- HY-W103960
-
|
|
Others
|
Metabolic Disease
|
|
Mirabegron impurity-1 is a potent and selective
β3- adrenergic receptor agonist. Mirabegron impurity-1
has the activity of inhibiting metabolism. Mirabegron impurity-1 can be used in
the study of the treatment of bladder impurity .
|
-
- HY-P1325
-
|
((Cys31, Nva 34)-Neuropeptide Y (27-36))2
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BWX 46 (((Cys31, Nva 34)-Neuropeptide Y (27-36))2) is a selective Y5 receptor agonist with an IC50 value of 0.85 nM. BWX 46 can inhibit the synthesis of cAMP in Y5 cells .
|
-
- HY-19006
-
|
|
Others
|
Neurological Disease
|
|
ZK-91296 is a GABA receptor agonist with anxiolytic activity. ZK-91296 can reduce anxiety in animals without causing sedation. ZK-91296 may have pharmacological selectivity for interaction with specific types of benzodiazepine receptors .
|
-
- HY-157425
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
|
-
- HY-100490
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-P1322A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats .
|
-
![[D-Trp34]-Neuropeptide Y TFA](//file.medchemexpress.eu/product_pic/hy-p1322a.gif)
- HY-100490B
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-115644
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties .
|
-
- HY-107678
-
|
WAY-317538
|
nAChR
|
Neurological Disease
|
|
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
|
-
- 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-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-15388
-
|
AGN 190168
|
RAR/RXR
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene 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-18978
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions .
|
-
- HY-70081A
-
|
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-109083
-
|
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research .
|
-
- HY-111021
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
|
-
- HY-100999
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-12720A
-
|
ALO 2145
|
Adrenergic Receptor
|
Neurological Disease
|
|
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid .
|
-
- HY-P3124A
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly .
|
-
- HY-P3124
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly .
|
-
- HY-117103
-
|
INT131
|
PPAR
|
Metabolic Disease
|
|
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM) .
|
-
- HY-111021A
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
|
-
- HY-103302
-
|
|
CGRP Receptor
|
Endocrinology
|
|
SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis .
|
-
- HY-110202
-
-
- HY-108571
-
|
|
PPAR
|
Metabolic Disease
|
|
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway .
|
-
- HY-108353
-
-
- HY-103092
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research .
|
-
- HY-118069
-
-
- HY-P4678
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
(Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
|
-
- HY-P4678A
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
(Phe2,Orn8)-Oxytocin acetate is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin acetate induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
|
-
- HY-149853
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AD186 is a potent and selective S1R agonist with Kis of 2.7, 27 nM for S1R and S2R, respectively. AD186 fully reverses the antiallodynic effect of BD-1063 (HY-18101A) .
|
-
- HY-161107
-
|
|
GPR84
|
Inflammation/Immunology
|
|
OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .
|
-
- HY-B0374AS
-
-
- HY-B1816
-
|
M&B 22948
|
Phosphodiesterase (PDE)
GPR35
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .
|
-
- HY-P1390A
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors .
|
-
![d[Cha4]-AVP TFA](//file.medchemexpress.eu/product_pic/hy-p1390a.gif)
- HY-103105
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
|
-
- HY-155484
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research .
|
-
- HY-B0468
-
|
Isoproterenol hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- HY-13736A
-
|
CV205-502 hydrochloride
|
Dopamine Receptor
Akt
|
Neurological Disease
Cancer
|
|
Quinagolide hydrochloride (CV205-502 hydrochloride) is a selective and orally active dopamine D2 receptor agonist. Quinagolide hydrochloride is an inhibitor of prolactin. Quinagolide hydrochloride down-regulates AKT levels and its phosphorylation. Quinagolide hydrochloride shows antitumor effects, it can be used for the research of cancer .
|
-
- HY-P0185
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
-
- HY-19334
-
-
- HY-110000
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
(+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.
|
-
- HY-110120
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect .
|
-
- HY-B0976
-
|
Th-1165; Phenoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-14304A
-
|
MJ 9184 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist . Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM . Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits .
|
-
- HY-P1338A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
-
- HY-136238
-
-
- 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-122124
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CAY10583 is a potent and selective full Leukotriene B4 receptor type 2 (BLT2) agonist. CAY10583 directly promotes keratinocyte migration in vitro and accelerates wound closure in vivo. CAY10583 is a promising pharmaceutical agent for diabetic wounds .
|
-
- HY-102057
-
|
TD-8954
|
5-HT Receptor
|
Others
|
|
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
|
-
- HY-101327
-
|
Corwin; ICI 118587
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol has the potential for the research of arrhythmogenesis. Xamoterol has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-108654
-
|
|
P2Y Receptor
Apoptosis
|
Neurological Disease
|
|
PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM . PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis .
|
-
- HY-108353A
-
-
- HY-P0185A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
-
- HY-124571
-
|
|
GPR84
|
Inflammation/Immunology
|
|
ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120 .
|
-
- HY-100904
-
|
2 BFI
|
Imidazoline Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI) .
|
-
- HY-153963
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- 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-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-B0383AS2
-
-
- HY-137608
-
|
UDP-β-S
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Uridine 5'-O-thiodiphosphate (UDP-β-S) is a stable analog of UDP. As a selective agonist of P2Y6 receptor, Uridine 5'-O-thiodiphosphate has higher metabolic stability and can be used in the study of cardiovascular diseases .
|
-
- HY-12199BS
-
|
Ciproxidine-d5 hydrochloride; BF 2649-d5 hydrochloride
|
Histamine Receptor
Isotope-Labeled Compounds
|
Neurological Disease
Endocrinology
|
|
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
|
-
- HY-109075
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Tasipimidine is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 for human α2A-adrenoceptors. Tasipimidine can be utilized in research related to situational anxiety and fear .
|
-
- HY-B1021
-
|
|
Free Fatty Acid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Vincamine?is a monoterpenoid indole alkaloid extracted from the?Madagascar periwinkle. Vincamine?is a peripheral?vasodilator?and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine?is a?GPR40?agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS).?Vincamine?improves glucose homeostasis?in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
|
-
- HY-100490A
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- 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-19752A
-
|
CID-25010775
|
mAChR
|
Neurological Disease
|
|
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .
|
-
- HY-14899
-
|
CP-544326
|
Prostaglandin Receptor
|
Endocrinology
|
|
Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors .
|
-
- HY-12844
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .
|
-
- HY-P1340
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
-
![[Ala11,D-Leu15]-Orexin B(human)](//file.medchemexpress.eu/product_pic/hy-p1340.gif)
- HY-P1301
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
![[Arg14,Lys15]Nociceptin](//file.medchemexpress.eu/product_pic/hy-p1301.gif)
- HY-123297
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .
|
-
- HY-17034AR
-
|
(+)-Medetomidine hydrochloride (Standard); (S)-Medetomidine hydrochloride (Standard)
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
- HY-12719R
-
|
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
|
Dexmedetomidine (Standard) is the analytical standard of Dexmedetomidine. This product is intended for research and analytical applications. Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .
|
-
- HY-14558
-
|
SM-3997
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .
|
-
- HY-B0180B
-
-
- HY-B0180A
-
|
R 837 hydrochloride
|
Toll-like Receptor (TLR)
Autophagy
SARS-CoV
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19 .
|
-
- HY-100488
-
|
|
Cannabinoid Receptor
|
Cancer
|
|
Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties .
|
-
- HY-B0180
-
-
- HY-12222S
-
|
INT-747-d5; 6-ECDCA-d5; 6-Ethylchenodeoxycholic acid-d5
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
|
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-136577
-
-
- HY-121653
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects .
|
-
- HY-103187
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype . HEMADO 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-108015
-
|
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
|
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect .
|
-
- 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-107413
-
|
BMS-649
|
RAR/RXR
|
Cancer
|
|
SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element .
|
-
- HY-125976
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM) .
|
-
- HY-12222S1
-
|
|
FXR
Autophagy
|
Others
|
|
Obeticholic Acid-d4 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
|
-
- 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-110053
-
|
SM-3997 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms .
|
-
- HY-103331
-
-
- HY-P3498
-
|
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-10475G
-
|
CD336; NSC608001; Ro 40-6055
|
RAR/RXR
|
Cancer
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
|
-
- HY-106316
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures .
|
-
- HY-101079
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
|
-
- HY-135021
-
|
|
5-HT Receptor
|
Others
|
|
3,4-Dihydro Naratriptan is a serotonin 5-HT1-receptor agonist. 3,4-Dihydro Naratriptan exhibits selective vasoconstrictor activity. 3,4-Dihydro Naratriptan can be used for migraine diseases research .
|
-
- HY-W010655
-
|
TAK-875 hemihydrate
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](//file.medchemexpress.eu/product_pic/hy-p10148.gif)
- HY-B0418AR
-
|
R-18553 hydrochloride (Standard)
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-B0584R
-
|
Fluprostenol isopropyl ester(Standard); AL6221(Standard); Flu-Ipr (Standard)
|
Prostaglandin Receptor
|
Endocrinology
|
|
Travoprost (Standard) is the analytical standard of Travoprost. This product is intended for research and analytical applications. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
|
-
- HY-114385
-
|
13,14-epoxy Fluprostenol isopropyl ester
|
Others
|
Others
|
|
13,14-epoxy Travoprost (13,14-epoxy Fluprostenol isopropyl ester) is a mixture of diastereomeric epoxides generated during production of Travoprost (HY-B0584). Travoprost is a selective agonist for prostaglandin F receptor, which exhibits an ocular hypotensive efficacy .
|
-
- HY-113616
-
|
|
mAChR
MARCKS
|
Neurological Disease
|
|
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .
|
-
- HY-121653B
-
|
DU-29373
|
5-HT Receptor
|
Neurological Disease
|
|
Flesinoxan hydrochloride is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan hydrochloride also has effective anxiolytic/antidepressant effects .
|
-
- HY-13225A
-
|
RJR-2403; (E)-Metanicotine
|
nAChR
|
Neurological Disease
|
|
Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .
|
-
- HY-17386
-
-
- HY-13221
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
BRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors .
|
-
- HY-14813
-
|
SA4503; AGY 94806
|
Sigma Receptor
|
Neurological Disease
|
|
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
|
-
- HY-A0039S
-
|
UK-116044-d3
|
5-HT Receptor
|
Neurological Disease
|
|
Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
|
-
- HY-N6642
-
|
|
PPAR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
|
-
- HY-115682
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Others
|
|
(S)-ZINC-3573 is an inactive enantiomer of ZINC-3573. (R)-ZINC-3573 is a selective MRGPRX2 agonist. (S)-ZINC-3573 and (R)-ZINC3573 are effective and internally controlled probe-pairs for investigating the biology of primate-exclusive receptor .
|
-
- HY-19360
-
|
SHB 286; CP-34089; ZK-57671
|
Prostaglandin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Sulprostone (SHB 286) is a potent and selective EP3 receptor agonist. Sulprostone (SHB 286) is a prostaglandin E2 (PGE2) analogue and has antiulcer and nonsteroidal abortifacient effects. Sulprostone has potential for the research of pregnancy termination and hemorrhages during delivery .
|
-
- HY-17386A
-
-
- HY-P0198B
-
-
![[D-Arg25]-Neuropeptide Y (human)](//file.medchemexpress.eu/product_pic/hy-p0198b.gif)
- HY-19933
-
|
MK-4618
|
Adrenergic Receptor
|
Others
|
|
Vibegron (MK-4618) is a potent, highly selective and orally active β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder .
|
-
- HY-103416
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor .
|
-
- HY-139485
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure .
|
-
- HY-P0208
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects .
|
-
![[Leu31,Pro34]-Neuropeptide Y (porcine)](//file.medchemexpress.eu/product_pic/hy-p0208.gif)
- HY-119515
-
|
(R)-(-)-Denopamine; TA-064
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Denopamine ((R)-(-)-Denopamine) is an orally active, selective β1-adrenergic agonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects .
|
-
- HY-12413A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models .
|
-
- HY-109075A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Tasipimidine sulfate is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 against human α2A-adrenoceptor. Tasipimidine sulfate can be used for situational anxiety and fear research .
|
-
- HY-17386B
-
-
- HY-103180
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs) .
|
-
- 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-100904A
-
|
2 BFI free base
|
Imidazoline Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RX 801077 (2 BFI free base) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 shows anti-inflammation and neuroprotection. RX 801077 has the potential for the research of traumatic brain injury (TBI) .
|
-
- HY-13221A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
BRL 54443 (MALEATE) is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors .
|
-
- HY-108901
-
|
|
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Formoterol hemifumarate hydrate is a selective, long-acting beta 2-adrenoceptor agonist. Formoterol is a bronchodilator used for the research of the asthma and chronic obstructive pulmonary disease (COPD). Formoterol hemifumarate hydrate induces mitochondrial biogenesis and promotes cognitive recovery after traumatic brain injury .
|
-
- HY-B1298
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Methoxamine hydrochloride is a selective alpha1-adrenergic receptor agonist. Methoxamine hydrochloride causes vasoconstriction and increased peripheral vascular resistance . Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery .
|
-
- HY-B1298A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methoxamine is a selective alpha1-adrenergic receptor agonist. Methoxamine causes vasoconstriction and increased peripheral vascular resistance . Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery .
|
-
- HY-B1614
-
-
- 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-P1340A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
-
![[Ala11,D-Leu15]-Orexin B(human) TFA](//file.medchemexpress.eu/product_pic/hy-p1340a.gif)
- HY-P1300
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
![[(pF)Phe4]Nociceptin(1-13)NH2](//file.medchemexpress.eu/product_pic/hy-p1300.gif)
- HY-P1301A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
![[Arg14,Lys15]Nociceptin TFA](//file.medchemexpress.eu/product_pic/hy-p1301a.gif)
- HY-128686
-
KAG-308
1 Publications Verification
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor .
|
-
- HY-17034AS
-
|
(+)-Medetomidine-13C,d3 hydrochloride; (S)-Medetomidine-13C,d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
|
-
- HY-107676A
-
|
|
nAChR
|
Neurological Disease
|
|
SIB-1553A free base is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A free base is also a selective neuronal nAChR ligand. SIB-1553A free base is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders .
|
-
- 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-100490S
-
|
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
- HY-119222
-
|
|
GPR109A
|
Metabolic Disease
|
|
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia . GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-115831
-
|
S1P1 agonist 3
|
LPL Receptor
|
Cardiovascular Disease
|
|
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .
|
-
- HY-119222A
-
|
|
GPR109A
|
Metabolic Disease
|
|
GSK256073 tris is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 tris acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia . GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-130179
-
|
|
Apoptosis
Others
|
Neurological Disease
|
|
RC-33 hydrochloride is a selective and metabolically stable σ? receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ? receptor with similar affinity and show almost equal effectiveness as σ? receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .
|
-
- HY-13956S
-
|
U 72107-d4
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
|
-
- HY-124581
-
|
|
PPAR
|
Metabolic Disease
|
|
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes .
|
-
- HY-120528
-
-
- HY-100689
-
|
PPT
|
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%) .
|
-
- HY-117516
-
|
|
REV-ERB
|
Neurological Disease
Metabolic Disease
|
|
SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders .
|
-
- HY-120528A
-
-
- 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-B0976A
-
|
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-107514
-
|
|
mGluR
|
Neurological Disease
|
|
(RS)-PPG is a potent and selective agonist for group III mGluRs. The EC50s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity .
|
-
- HY-P1214
-
-
- HY-136578
-
-
- HY-141514
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide .
|
-
- HY-15831
-
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease .
|
-
- 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-P1096
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
|
-
- HY-107666
-
-
- HY-108448
-
|
OLDA
|
TRP Channel
|
Cardiovascular Disease
|
|
N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1 .
|
-
- HY-108527
-
|
|
RAR/RXR
|
Cancer
|
|
CD1530 is a selective RARγ agonist with an Kd of 150 nM . CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma .
|
-
- HY-101327A
-
|
Corwin hemifumarate; ICI 118587 hemifumarate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-101317
-
|
SB-205607 dihydrobromide
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke .
|
-
- HY-126910
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
|
-
- HY-115462
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
PGN-9856 is a selective and high affinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
|
-
- 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-13956C
-
|
(R)-U 72107
|
PPAR
|
Neurological Disease
|
|
(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
|
-
- HY-18060A
-
|
TC-5619 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Bradanicline hydrochloride (TC-5619 hydrochloride) is the hydrochloride salt form of Bradanicline (HY-18060). Bradanicline hydrochloride is a selective agonist for α7 nicotinic acetylcholine receptor (nAChR), with EC50 of 17 nM for human α7 nAChR and Ki of 1.4 nM. Bradanicline hydrochloride is used for the research of cognitive disorders and schizophrenia .
|
-
- HY-B1216R
-
|
|
Sigma Receptor
|
Cardiovascular Disease
Others
Neurological Disease
|
|
Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .
|
-
- HY-106889
-
|
YM435 free base
|
Dopamine Receptor
|
Others
|
|
Zelandopam free base (YM435 free base) is an orally active and selective agonist of the dopamine D1 receptor. Zelandopam free base possesses potent renal vasodilatory properties and can effectively alleviate cisplatin (HY-17394)-induced acute renal failure .
|
-
- 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-113749
-
|
|
Others
|
Inflammation/Immunology
|
|
L-Mabuterol hydrochloride is a selective β2-adrenergic receptor agonist with bronchodilator activity. L-Mabuterol hydrochloride can improve respiratory function and relieve asthma symptoms. L-Mabuterol hydrochloride also shows potential efficacy in the management of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-P2242A
-
|
|
Melanocortin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects .
|
-
- HY-103565
-
|
|
mGluR
|
Neurological Disease
|
|
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-P1300A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
![[(pF)Phe4]Nociceptin(1-13)NH2 TFA](//file.medchemexpress.eu/product_pic/hy-p1300a.gif)
- HY-120511
-
KNT-127
1 Publications Verification
|
Opioid Receptor
|
Neurological Disease
|
|
KNT-127 is a potent and selective δ-opioid receptor agonist effective by systemic administration. KNT-127 shows selectivity for the δ-receptor (Ki 0f 21.3, 0.16, 153 nM for opioid μ-, δ-, and κ-receptors, respectively). KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. Antidepressant-like effects .
|
-
- 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-B1052S
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Lofexidine-d4 (hydrochloride) (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride. Lofexidine hydrochloride is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
|
-
- HY-19358
-
|
2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects .
|
-
- HY-19358A
-
|
2-Methyl-5-hydroxytryptamine hydrochloride; 2-Methylserotonin hydrochloride; 2-Me-HT hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine hydrochloride) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT hydrochloride is shown to display anti-depressive-like effects .
|
-
- HY-19358B
-
|
2-Methyl-5-hydroxytryptamine maleate; 2-Methylserotonin maleate; 2-Me-HT maleate
|
5-HT Receptor
|
Neurological Disease
|
|
2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT maleate is shown to display anti-depressive-like effects .
|
-
- HY-P1112
-
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1316
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
|
-
- HY-P1316A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
|
-
- HY-P2454
-
|
|
Bacterial
|
Infection
|
|
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent .
|
-
- HY-131180
-
|
LAR-1219
|
Formyl Peptide Receptor (FPR)
|
Cardiovascular Disease
|
|
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure .
|
-
- HY-P3057
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension .
|
-
![[D-Trp11]-Neurotensin](//file.medchemexpress.eu/product_pic/hy-p3057.gif)
- HY-B1696A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate hydrochloride is an ethyl ester hydrochloride proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research .
|
-
- HY-138879
-
|
|
nAChR
|
Neurological Disease
|
|
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
|
-
- HY-116565
-
|
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
|
-
- HY-145698
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR .
|
-
- HY-121852
-
|
SCH-225336
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
|
-
- HY-B1696
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate is an ethyl ester proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research .
|
-
- HY-P3433
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively .
|
-
- HY-150067
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity .
|
-
- HY-113616A
-
|
|
MARCKS
mAChR
|
Neurological Disease
|
|
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .
|
-
- HY-155100
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. BI 7446 can activate all five STING variants in cells and induce tumor-specific immune-mediated tumor rejection. BI 7446 can be used for immuno-oncology research .
|
-
- HY-118806
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
|
-
- HY-116586A
-
|
|
mAChR
Sigma Receptor
|
Neurological Disease
|
|
(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
|
-
- 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-111918
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
A71378 is a selectivity CCK-A receptor agonist the IC50 values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC50 = 0.16 nM) and ileal muscle contraction (EC50 = 3.7 nM) .
|
-
- HY-113820
-
|
|
PPAR
|
Metabolic Disease
|
|
AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
|
-
- HY-76772
-
|
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
|
-
- HY-70020B
-
|
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
|
-
- HY-17043S
-
-
- HY-B0471S
-
|
(R)-(-)-Phenylephrine-d3 (hydrochloride); L-Phenylephrine-d3 (hydrochloride)
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
|
-
- HY-17043S1
-
-
- HY-113854
-
|
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
|
AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
|
-
- HY-119744
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties .
|
-
- HY-W020468
-
|
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue .
|
-
- HY-14611
-
|
DFB
|
mGluR
|
Neurological Disease
|
|
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
|
-
- HY-P1214A
-
-
- HY-B0154S
-
-
- HY-W016868
-
|
|
Others
|
Metabolic Disease
|
|
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity .
|
-
- HY-B0154S1
-
-
- HY-B0471S3
-
-
- HY-116820
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
|
-
- HY-103144
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY 629 hydrochloride is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 hydrochloride decreases feeding behavior .
|
-
- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
|
-
- HY-155556
-
|
|
ClpP
|
Cancer
|
|
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
|
-
- HY-18941B
-
|
(rel)-LY354740; (rel)-Eglumetad
|
mGluR
|
Neurological Disease
|
|
(rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively .
|
-
- HY-14157
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms .
|
-
- HY-117376
-
|
UAB30
|
RAR/RXR
|
Cancer
|
|
(all-E)-UAB30 (UAB30) is an retinoid X receptor (RXR) selective agonist.(all-E)-UAB30 shows anti-proliferation activity for MyLa, HuT 78, and HH cells with the IC50 of 34.7, 5.1, and 22.4 μM respectively .
|
-
- HY-118010A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
- HY-W131725
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
- HY-103144A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY 629 is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 decreases feeding behavior .
|
-
- HY-121671
-
|
|
Others
|
Neurological Disease
|
|
TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models .
|
-
- HY-104037A
-
|
LYC-55716 sodium
|
ROR
|
Cancer
|
|
Cintirorgon sodium is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon sodium (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
|
-
- HY-14157A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms .
|
-
- HY-14933
-
|
ERB-041
|
Estrogen Receptor/ERR
Wnt
Apoptosis
|
Cancer
|
|
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
|
-
- HY-101358
-
|
AH-002
|
Melatonin Receptor
|
Neurological Disease
|
|
8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity .
|
-
- HY-101202
-
|
NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
|
-
- HY-10063
-
|
TC-1734; ACD3480
|
nAChR
|
Neurological Disease
|
|
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
|
-
- HY-119103
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research .
|
-
- HY-16734A
-
|
MT-1303 hydrochloride
|
LPL Receptor
|
Cancer
|
|
Amiselimod hydrochloride is an orally active novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod-P shows potent and high selectivity for S1P1 and S1P5 but with minimal agonist activity for S1P4 and no distinct agonist activity for S1P2 or S1P3. Amiselimod hydrochloride is promising for research of autoimmune diseases .
|
-
- HY-14330
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- HY-103409
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- 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 .
|
-
- HY-14262
-
|
EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
|
-
- HY-10473
-
|
KB2115
|
Thyroid Hormone Receptor
|
Metabolic Disease
Endocrinology
|
|
Eprotirome (KB2115) is a liver-selective thyroid hormone receptor (TR) agonist. KB2115 has modestly higher affinity for TRβ than for TRα. Eprotirome reduces low-density lipoprotein (LDL) cholesterol concentrations. Eprotirome can be used for dyslipidemias and obesity research .
|
-
- HY-101176
-
|
|
Melatonin Receptor
|
Cancer
|
|
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
|
-
- HY-P1112A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
-
- HY-117066
-
CL075
2 Publications Verification
3M002
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively .
|
-
- HY-134130
-
|
|
Integrin
|
Inflammation/Immunology
|
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM .
|
-
- HY-124283A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors .
|
-
- HY-P3155
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R .
|
-
- HY-109155
-
|
CRN00808
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors .
|
-
- HY-107046
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research .
|
-
- HY-119226
-
|
|
mAChR
|
Neurological Disease
|
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
|
-
- HY-B0225AS
-
|
L-(-)-α-Methyldopa-d3 hydrochloride; MK-351-d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system[1][2].
|
-
- HY-B0471S2
-
-
- HY-B1481
-
|
Isoetarine mesylate
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
|
-
- HY-B1481A
-
|
Isoetarine
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
|
-
- HY-108656A
-
|
|
P2Y Receptor
Arrestin
|
Cardiovascular Disease
|
|
MRS2365 trisodium is a potent and selective P2Y1 receptor (EC50=0.4 nM)/[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity .
|
-
- HY-B0584A
-
|
5,6-trans-Fluprostenol isopropyl ester; 5,6-trans-AL6221; 5,6-trans-Flu-Ipr
|
Others
|
Endocrinology
|
|
5,6-trans-Travoprost is the isomer of Travoprost (HY-B0584), and can be used as an experimental control. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
|
-
- HY-111271B
-
|
|
Others
|
Inflammation/Immunology
Endocrinology
|
|
(R)-L 888607 is the isomer of L 888607 (HY-111271), and can be used as an experimental control. L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
|
-
- HY-163277
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
|
-
- HY-A0168A
-
|
CVT-3146 hydrate
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Regadenoson hydrate (NSC 169186) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
|
-
- 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-14356
-
-
- HY-162728
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .
|
-
- HY-106973A
-
|
CHF 1035
|
Dopamine Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nolomirole (CHF 1035) hydrochloride is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output .
|
-
- HY-109155A
-
|
CRN00808 hydrochloride
|
Somatostatin Receptor
|
Neurological Disease
Endocrinology
|
|
Paltusotine (CRN00808) hydrochloride is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine hydrochloride has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine hydrochloride can be used in research on acromegaly and neuroendocrine tumors .
|
-
- HY-106756
-
|
U-62066
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-124959
-
|
U-62066 mesylate
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-70020
-
|
AF102B
|
mAChR
|
Neurological Disease
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
|
-
- HY-13044
-
-
- HY-13956
-
|
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
|
-
- HY-10426
-
|
|
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
|
-
- HY-A0168
-
|
CVT-3146
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
|
-
- HY-104037
-
|
LYC-55716
|
ROR
|
Cancer
|
|
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
|
-
- HY-100256
-
|
CD5789
|
RAR/RXR
Autophagy
|
Inflammation/Immunology
|
|
Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively .
|
-
- HY-111615
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-105634A
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-124071
-
|
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders .
|
-
- HY-111793
-
|
|
CXCR
|
Neurological Disease
|
|
NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo .
|
-
- HY-108497
-
|
|
Somatostatin Receptor
|
Neurological Disease
Cancer
|
|
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
|
-
- HY-111793A
-
|
|
CXCR
|
Neurological Disease
|
|
NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo .
|
-
- HY-12598
-
|
|
mGluR
|
Neurological Disease
|
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively . (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia .
|
-
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-110173
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo .
|
-
- 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-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-116699
-
|
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions .
|
-
- HY-136181A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-136181
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- 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-B0180S
-
-
- HY-110094
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors .
|
-
- HY-116565A
-
|
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
|
-
- HY-B0180S1
-
-
- 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-13956B
-
|
U 72107 potassium
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
|
-
- 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-18941C
-
|
LY354740 hydrochloride; Eglumetad hydrochloride
|
mGluR
|
Neurological Disease
|
|
Eglumegad (LY354740) hydrochloride is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. Eglumegad hydrochloride protects neurons from NMDA toxicity. Eglumegad hydrochloride has anxiolytic- and antipsychotic-like effects .
|
-
- HY-103292
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
[Phe8Ψ(CH-NH)Arg9]-Bradykinin is a selective Bradykinin receptor B2 agonist (not cleaved by protein kinase I/II). [Phe8Ψ(CH-NH)Arg9]-Bradykinin has potential for the research of hypertension .
|
-
![[Phe8Ψ(CH-NH)Arg9]-Bradykinin](//file.medchemexpress.eu/product_pic/hy-103292.gif)
- HY-117356B
-
|
|
P2Y Receptor
NF-κB
ERK
|
Cardiovascular Disease
|
|
MRS2693 trisodium is a selective P2Y6 agonist with an EC50 value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model .
|
-
- HY-161246
-
|
|
Others
|
Neurological Disease
|
|
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
|
-
- HY-160715
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
BNT411 is a selective TLR7 agonist that can induce the release of IFNa both in vivo and in vitro. BNT411 has anticancer activity and can be used in cancer research, including non-small cell lung cancer, pancreatic cancer, and untreated extensive-stage small cell lung cancer (ES-SCLC) .
|
-
- HY-17043R
-
|
|
Dengue virus
Flavivirus
Histamine Receptor
|
Infection
Inflammation/Immunology
Endocrinology
Cancer
|
|
Loratadine (Standard) is the analytical standard of Loratadine. This product is intended for research and analytical applications. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
|
-
- HY-115357
-
|
|
PPAR
|
Metabolic Disease
|
|
BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC50 of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides .
|
-
- HY-139120
-
|
19(R)-Hydroxy PGE2; 19(R)-OH PGE2
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
19(R)-hydroxy Prostaglandin E2 (19(R)-hydroxy PGE2) is found in the semen of primates, including man. It is a potent smooth muscle relaxant and a selective agonist for the EP2 receptor. It has an EC50 value of 200 nM for relaxing cat tracheal rings which express EP2 receptors.
|
-
- 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-B0468S
-
|
Isoproterenol-d7 hydrochloride
|
Isotope-Labeled Compounds
Endogenous Metabolite
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- 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-122147
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
L-644698 is a potent and selective human recombinant prostaglandin D2 (PGD2) receptor (hDP) agonist with Ki values of 0.9, 267, 3730, 9280 nM for hDP, hEP2, hEP3, hEP4, respectively. L-644698 induces cyclic AMP production with an EC50 value of 0.5 nM .
|
-
- HY-P1033S
-
-
![[Pyr1]-Apelin-13, Gly(15N) TFA](//file.medchemexpress.eu/product_pic/hy-p1033s.gif)
- HY-15451R
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 (Standard) is the analytical standard of MDA 19. This product is intended for research and analytical applications. MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-B0154R
-
-
- HY-B0471R
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Phenylephrine (hydrochloride) (Standard) is the analytical standard of Phenylephrine (hydrochloride). This product is intended for research and analytical applications. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
|
-
- HY-162726
-
|
|
Interleukin Related
|
Cancer
|
|
GCS-11 is a powerful natural killer T (NKT) cell agonist. It boosts the production of IFN-γ and IL-4, with a particular selectivity for IFN-γ. GCS-11 exhibits anticancer activity. GCS-11 has the potential for research into cancer immunotherapies or vaccine development as a promising adjuvant .
|
-
- HY-B0225BR
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa (hydrate) (Standard) is the analytical standard of Methyldopa (hydrate). This product is intended for research and analytical applications. Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
|
-
- HY-114794R
-
|
|
Adrenergic Receptor
Drug Metabolite
|
Cardiovascular Disease
|
|
Desglymidodrine (Standard) is the analytical standard of Desglymidodrine. This product is intended for research and analytical applications. Desglymidodrine (ST 1059), the active metabolite of Midodrine (HY-12749), is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure .
|
-
- HY-145463
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
α-Methylserotonin is a potent and selective agonist of 5-HT2 receptor.α-Methylserotonin is an analogue of serotonin formed in vivo from α-methyltryptophan.α-Methylserotonin mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
|
-
- 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 .
|
-
- HY-P1206
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
|
-
- 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 .
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-P1117
-
|
|
Formyl Peptide Receptor (FPR)
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK1 potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity .
|
-
- HY-B1021R
-
|
|
Free Fatty Acid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Vincamine (Standard) is the analytical standard of Vincamine. This product is intended for research and analytical applications. Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
|
-
- 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 .
|
-
- HY-137295
-
|
|
PKC
Apoptosis
|
Inflammation/Immunology
|
|
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
|
-
- HY-19996
-
AH-7614
2 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-110220
-
|
|
TRP Channel
|
Neurological Disease
|
|
CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research .
|
-
- HY-103565A
-
|
|
mGluR
|
Neurological Disease
|
|
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-116461
-
|
CID2440433
|
GPR55
|
Neurological Disease
|
|
ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55 . ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro .
|
-
- HY-P5372
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
|
-
- HY-14422
-
|
|
ROR
|
Cancer
|
|
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
|
-
- HY-B0084
-
|
STS 557
|
Progesterone Receptor
|
Endocrinology
|
|
Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
|
-
- HY-14302
-
|
GR33343X
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
|
-
- HY-B0007
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
|
-
- HY-13591
-
|
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
|
-
- HY-B0471S1
-
|
(R)-(-)-Phenylephrine-2,4,6-d3 (hydrochloride); L-Phenylephrine-2,4,6-d3 (hydrochloride)
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
|
-
- HY-P1744
-
-
- HY-12150
-
CCMI
1 Publications Verification
AVL-3288; UCI-4083
|
nAChR
|
Neurological Disease
|
|
CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
|
-
- HY-101364
-
|
|
mGluR
NF-κB
ERK
Akt
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways .
|
-
- HY-101364A
-
|
|
mGluR
NF-κB
ERK
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways. .
|
-
- 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-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- 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-123352
-
|
(+)-ZK 216348
|
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects .
|
-
- HY-111226
-
GSK5182
2 Publications Verification
|
Estrogen Receptor/ERR
Reactive Oxygen Species
|
Cardiovascular Disease
Cancer
|
|
GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .
|
-
- HY-100448A
-
|
|
Prostaglandin Receptor
TGF-beta/Smad
|
Endocrinology
|
|
Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling .
|
-
- HY-103558
-
|
|
mGluR
|
Neurological Disease
|
|
LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects .
|
-
- HY-103133
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex . WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects .
|
-
- 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-111366
-
|
|
ROR
|
Inflammation/Immunology
|
|
CD12681 (compound 14) is a potent and selective RORγ inverse agonist with IC50 of 19 nM and 10 nM for RORγ GAL4 and CD4-IL-17 cells, respectively. CD12681 decreases the IL-17 inflammatory cell recruitment. CD12681 has the potential for the research of psoriasis .
|
-
- HY-B0007C
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .
|
-
- HY-17416A
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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-
- HY-17416
-
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|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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-
- HY-114910
-
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|
Prostaglandin Receptor
|
Cancer
|
|
11-Deoxy Prostaglandin E2 is a selective agonist of EP4 with an EC50 of 0.66 nM. 11-Deoxy Prostaglandin E2 is an analog of prostaglandin E2. 11-Deoxy Prostaglandin E2 can be used in study bone healing, heart failure, and other receptor associated conditions .
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-
- HY-12720AR
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Apraclonidine (hydrochloride) (Standard) is the analytical standard of Apraclonidine (hydrochloride). This product is intended for research and analytical applications. Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid .
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-
- HY-15388R
-
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|
RAR/RXR
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Tazarotene (Standard) is the analytical standard of Tazarotene. This product is intended for research and analytical applications. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene 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-120531
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
UR-PI376 is a potent and selective histamine H4 receptor (H4R) agonist with a pEC50 value of 7.47. UR-PI376 shows negligible hH1R and hH2R activities and moderate inverse agonistic activity at the hH3R .
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-
- HY-B0468R
-
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|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Isoprenaline (hydrochloride) (Standard) is the analytical standard of Isoprenaline (hydrochloride). This product is intended for research and analytical applications. Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
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-
- HY-163996
-
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|
GLP Receptor
|
Metabolic Disease
|
|
DD202-114 is a potent and selective GLP1R agonist. DD202-114 promots cAMP accumulation. DD202-114 reduces blood glucose levels and food intake. DD202-114 has the potential for the research of type 2 diabetes (T2DM) and obesity .
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-
- 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-19436A
-
|
GW 427353B
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Solabegron hydrochloride is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM . Solabegron hydrochloride (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .
|
-
- HY-A0168S
-
|
CVT-3146-d3
|
Adenosine Receptor
|
Cardiovascular Disease
Cancer
|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
|
-
- 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-P1117A
-
|
|
Formyl Peptide Receptor (FPR)
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
MMK1 TFA is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 TFA is a potent chemotactic and calcium-mobilizing agonist. MMK1 TFA potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 TFA exerts anxiolytic-like activity .
|
-
- HY-15589
-
GW9508
5 Publications Verification
|
Free Fatty Acid Receptor
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
|
-
- HY-15340
-
|
LG268
|
RAR/RXR
Autophagy
|
Metabolic Disease
|
|
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
|
-
- HY-136207
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
|
-
- HY-105670
-
|
|
nAChR
|
Neurological Disease
|
|
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .
|
-
- HY-103521
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo .
|
-
- HY-105670B
-
|
|
nAChR
|
Neurological Disease
|
|
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .
|
-
- HY-A0014
-
|
TAK-375
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
|
-
- HY-17453
-
|
GR 33343X xinafoate
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
|
-
- HY-112603
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research .
|
-
- HY-13956S1
-
|
|
Isotope-Labeled Compounds
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
|
-
- HY-103186
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction .
|
-
- HY-19436
-
|
GW 427353
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM . Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .
|
-
- HY-19976
-
RN-1747
2 Publications Verification
|
TRP Channel
|
Cardiovascular Disease
|
|
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM .
|
-
- HY-101299A
-
|
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity . Dihydrexidine can stimulate YAP phosphorylation .
|
-
- HY-10232
-
THIP
1 Publications Verification
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
|
-
- HY-101299B
-
|
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity . Dihydrexidine hydrochloride can stimulate YAP phosphorylation .
|
-
- HY-P1131
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
-
- 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-135881
-
|
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM) .
|
-
- HY-131891
-
|
|
mAChR
|
Neurological Disease
|
|
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
|
-
- HY-14495
-
|
EX-1314
|
GHSR
|
Metabolic Disease
|
|
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents .
|
-
- HY-14495B
-
|
EX-1314 dihydrochloride
|
GHSR
|
Metabolic Disease
|
|
BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents .
|
-
- HY-101369
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BW-723C86 is a potent and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats .
|
-
- HY-112603A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research .
|
-
- HY-12959A
-
|
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
|
-
- HY-A0039
-
|
UK-116044
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .
|
-
- HY-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 .
|
-
- 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-15103
-
|
|
Androgen Receptor
Thyroid Hormone 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-141496
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity .
|
-
- HY-121859
-
|
|
Glucocorticoid Receptor
|
Metabolic Disease
|
|
RU28362 is a potent and selective glucocorticoid agonist. RU28362 increases the Bnip3 mRNA levels in neurons. RU28362 inhibits adrenocorticotrophic hormone (ACTH) and corticosterone secretion . RU28362 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-13338
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Mabuterol is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB .
|
-
- HY-107681
-
|
|
nAChR
|
Neurological Disease
|
|
SIB-1508Y is an orally active and selective nAChR agonist. SIB-1508Y has the potential to study parkinsonism . SIB-1508Y 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-122112
-
|
|
Sigma Receptor
|
Cancer
|
|
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-153963A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- 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-111582G
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .
|
-
- HY-W755295
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Mabuterol hydrochloride is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol hydrochloride inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol hydrochloride suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB .
|
-
- HY-158058
-
|
|
Toll-like Receptor (TLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-17386S1
-
-
- HY-162401
-
|
|
RXFP Receptor
|
Cardiovascular Disease
|
|
AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC50 > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research .
|
-
- HY-14558R
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone (Standard) is the analytical standard of Tandospirone. This product is intended for research and analytical applications. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .
|
-
- HY-17386R
-
-
- HY-B0180R
-
|
|
Toll-like Receptor (TLR)
Autophagy
SARS-CoV
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Imiquimod (Standard) is the analytical standard of Imiquimod. This product is intended for research and analytical applications. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
|
-
- HY-14915A
-
|
MN-221; KUR-1246
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Bedoradrine (MN-221) sulfate is a highly selective β2-adrenergic receptor agonist. Bedoradrine sulfate can effectively relieve airway spasm in asthma patients, dilate airway smooth muscle cells, reduce airway inflammation, and thus improve respiratory function. Bedoradrine sulfate can be used in research on asthma treatment .
|
-
- HY-163945
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
ZTA-261 is a highly selective and low toxic thyroid hormone receptor β subtype (THR-β) agonist (IC50=6.3 nM) that reduces body weight and visceral fat through a liothyronine (HY-A0070A) mediated pathway. ZTA-261 can be used in the study of lipid metabolism and obesity prevalence .
|
-
- HY-124950
-
|
GR114297A
|
Adrenergic Receptor
|
Others
|
|
Picumeterol (GR114297A) is a potent and selective β2-adrenoceptor agonist with bronchodilator and anti-bronchoconstrictor effects. Picumeterol produces long-lasting relaxation of airways smooth muscle both in vitro and in vivo. Picumeterol is cleared from plasma through a rapid and extensive hepatic metabolism. Picumeterol is proming for rasearch of asthma and related diseases .
|
-
- 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-148611
-
|
|
Others
|
Neurological Disease
|
|
NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases .
|
-
- HY-18723
-
|
|
Piezo Channel
Akt
ERK
Potassium Channel
|
Cardiovascular Disease
|
|
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .
|
-
- HY-14803
-
|
BMS-214778; VEC-162
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
|
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
|
-
- HY-12554
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
|
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
- 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-113756A
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor . Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes .
|
-
- HY-13717
-
|
IRX4204; NRX194204; VTP 194204
|
RAR/RXR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions .
|
-
- 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-12554A
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
|
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
- HY-111226A
-
|
|
Estrogen Receptor/ERR
Reactive Oxygen Species
|
Cardiovascular Disease
Cancer
|
|
(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM . GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma .
|
-
- HY-P1131A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 TFA is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617 TFA, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
-
- HY-P1397A
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
|
|
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
-
- HY-111615A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-131881
-
|
|
mAChR
|
Neurological Disease
|
|
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
|
-
- HY-12959
-
|
BAY x 3702 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects .
|
-
- HY-19884
-
|
RM-131; BIM-28131
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
-
- HY-103212
-
|
B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively . Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM) .
|
-
- HY-139783
-
|
|
Apoptosis
|
Others
|
|
3-Campholenyl-2-butanol, a synthetic sandalwood odorant, is a selective olfactory receptor OR2AT4 agonist. 3-Campholenyl-2-butanol prolongs human hair growth ex vivo by decreasing apoptosis and increasing production of the anagen-prolonging growth factor IGF-1 in the outer root sheath (ORS) .
|
-
- HY-145153
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
|
-
- HY-107648
-
|
|
mAChR
|
Inflammation/Immunology
|
|
McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis . McN-A-343 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-148250
-
|
|
iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission .
|
-
- HY-P3684
-
|
|
CRFR
|
Endocrinology
|
|
[DPro5] Corticotropin Releasing Factor, human, rat is a selective R2 agonist of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin. [DPro5] Corticotropin Releasing Factor, human, rat fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat .
|
-
![[DPro5] Corticotropin Releasing Factor, human, rat](//file.medchemexpress.eu/product_pic/hy-p3684.gif)
- HY-134440A
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene ATP, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .
|
-
- HY-N8264
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities .
|
-
- HY-123352A
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
(-)-ZK 216348 is the enantiomer of (+)-ZK 216348 (HY-123352). (+)-ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects .
|
-
- HY-103295
-
|
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors .
|
-
![Lys-[Des-Arg9]Bradykinin](//file.medchemexpress.eu/product_pic/hy-103295.gif)
- HY-P1016
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 1 2.
|
-
- HY-P1368
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
|
-
- HY-12554B
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
- HY-105670A
-
|
|
nAChR
|
Neurological Disease
|
|
PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For α3β4, α1β1γδ, α4β2 and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia .
|
-
- 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-109065
-
|
|
5-HT Receptor
|
Others
|
|
Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the 5-HT4 receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C) .
|
-
- HY-19425
-
|
|
PPAR
|
Metabolic Disease
|
|
NS-220 is an orally active PPARα agonist with high subtype selectivity, with EC50 values of 1.9×10 -8 M, 9.6×10 -6 M and >10 -4 M for PPARα, PPAR γ and PPARδ, respectively. NS-220 is used in the research for hyperlipidemia or metabolic disorders in type-2 diabetes .
|
-
- HY-118316
-
|
|
Others
|
Inflammation/Immunology
|
|
GSK223 is a quinazolinone NOD1 pathway inhibitor with potential anti-inflammatory activity. GSK223 can selectively inhibit IL-8 release under iE-DAP stimulation without affecting IL-8 secretion caused by TNF receptor, TLR2 or NOD2 agonists. GSK223 does not directly inhibit RIP2 kinase activity.
|
-
- HY-P1033S1
-
-
![[Pyr1]-Apelin-13, Pro(13C5,15N) TFA](//file.medchemexpress.eu/product_pic/hy-p1033s1.gif)
- HY-123328
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
AGN 191976 is a potent and selective thromboxane A2-sensitive (TP) receptor agonist with EC50 values of 0.23 nM and 24 nM in rat aorta and human platelets, respectively. AGN 191976 has potent IOP-lowering effects in dogs and monkeys. AGN 191976 can be used to study vascular biology and the role of thromboxane A2 in vascular function .
|
-
- HY-135392S
-
|
AC-279-d9 hydrochloride
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
|
-
- HY-W103960R
-
|
|
Others
|
Metabolic Disease
|
|
Mirabegron impurity-1 (Standard) is the analytical standard of Mirabegron impurity-1. This product is intended for research and analytical applications. Mirabegron impurity-1 is a potent and selective
β3- adrenergic receptor agonist. Mirabegron impurity-1
has the activity of inhibiting metabolism. Mirabegron impurity-1 can be used in
the study of the treatment of bladder impurity .
|
-
- HY-117090
-
|
(rac)-4,5-DHP-AMT
|
Others
|
Others
|
|
(rac)-AL-37350A ((rac)-4,5-DHP-AMT) is a 5-HT2 receptor agonist with intraocular pressure-lowering activity. (rac)-AL-37350A has high affinity and selectivity for the 5-HT2 receptor and effectively reduces intraocular pressure in conscious hypertensive cynomolgus monkeys.
|
-
- HY-14565
-
|
ABT-089
|
nAChR
|
Neurological Disease
|
|
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
|
-
- HY-14604
-
|
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
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-19674
-
|
SSR182289A free base
|
Thrombin
|
Cardiovascular Disease
|
|
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
|
-
- HY-14171
-
|
LGD1069
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
|
-
- HY-10569
-
|
ACT-128800
|
LPL Receptor
|
Inflammation/Immunology
|
|
Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-10435
-
|
(±)-SKF-82958; Chloro-APB
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
|
-
- HY-18100A
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-112061
-
|
8-Hydroxy-DPAT
|
5-HT Receptor
|
Neurological Disease
|
|
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
|
-
- HY-135119
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Salmeterol-d3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
|
-
- HY-16718
-
|
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
|
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
|
-
- HY-W010832
-
-
- HY-108652
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene-ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand . α,β-Methylene-ATP trisodium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .
|
-
- HY-103131
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy .
|
-
- HY-136527
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
|
-
- HY-103295A
-
|
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors .
|
-
![Lys-[Des-Arg9]Bradykinin TFA](//file.medchemexpress.eu/product_pic/hy-103295a.gif)
- HY-120645
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
|
-
- HY-19884A
-
|
RM-131 acetate; BIM-28131 acetate
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
-
- HY-134440
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand . α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .
|
-
- HY-16718A
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PF-00251802 hydrochloride
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Glucocorticoid Receptor
Cytochrome P450
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Inflammation/Immunology
Endocrinology
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Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
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- HY-108493
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LPL Receptor
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Inflammation/Immunology
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CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR .
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- HY-113962S
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- HY-134988
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FXR
Phosphatase
Cytochrome P450
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Inflammation/Immunology
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EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
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- HY-108675
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MMP
P2X Receptor
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Infection
Cancer
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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 .
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- HY-P1019
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction
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![[Ala1,3,11,15]-Endothelin (53-63)](//file.medchemexpress.eu/product_pic/hy-p1019.gif)
- HY-112597A
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REN001; HPP593
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PPAR
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Inflammation/Immunology
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Mavodelpar (REN001) is a selective PPARδ agonist. Mavodelpar suppresses glomerular injury and renal fibrosis. Mavodelpar can be used for the research of primary mitochondrial myopathies (PMM) and long-chain fatty acid oxidation disorders (LC-FAOD) . Mavodelpar 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-18100
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Sigma Receptor
Akt
NO Synthase
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Cardiovascular Disease
Neurological Disease
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PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
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- HY-123249
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GABA Receptor
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Neurological Disease
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HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 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-154985
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PPAR
Bombesin Receptor
ERK
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Metabolic Disease
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DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
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- HY-107668A
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nAChR
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Neurological Disease
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TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research .
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- HY-103291
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Bradykinin Receptor
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Inflammation/Immunology
Endocrinology
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Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings .
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![Sar-[D-Phe8]-des-Arg9-Bradykinin](//file.medchemexpress.eu/product_pic/hy-103291.gif)
- HY-P1368A
-
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Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA
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CRFR
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Endocrinology
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Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
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- HY-B0976AR
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Th-1165a (Standard); Phenoterol hydrobromide (Standard)
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Adrenergic Receptor
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Inflammation/Immunology
Endocrinology
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Fenoterol (hydrobromide) (Standard) is the analytical standard of Fenoterol (hydrobromide). This product is intended for research and analytical applications. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
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- HY-14262S1
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EMD 68843-d8; SB659746A-d8
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5-HT Receptor
Serotonin Transporter
Isotope-Labeled Compounds
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Neurological Disease
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Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-P10318
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GLP Receptor
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Endocrinology
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SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
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- HY-105017
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ATL 313; DE 112
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Adenosine Receptor
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Infection
Inflammation/Immunology
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Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .
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- HY-14262R
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5-HT Receptor
Serotonin Transporter
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Neurological Disease
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Vilazodone (Standard) is the analytical standard of Vilazodone. This product is intended for research and analytical applications. Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-107668
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nAChR
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Neurological Disease
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TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research .
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- HY-117971
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Others
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Others
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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.
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- HY-167824
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Others
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Neurological Disease
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SSR180711 is a potent and subtype-selective α7 agonist with activity in Alzheimer's disease and schizophrenia research. SSR180711 can be used to study subtypes of intracerebral hemorrhage associated with cerebral small vessel disease. SSR180711 shows potential in electrophysiological and behavioral studies to evaluate its effects on cognitive function. SSR180711 also has potential for studying cerebrovascular lesions and their effects .
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- HY-115857
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Others
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Neurological Disease
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SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
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- HY-15697
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TUG-770
3 Publications Verification
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Free Fatty Acid Receptor
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Metabolic Disease
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TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research . TUG-770 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-103142
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5-HT Receptor
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Neurological Disease
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AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia .
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- HY-17356
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PPAR
Cytochrome P450
Autophagy
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Cardiovascular Disease
Cancer
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Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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- HY-16673
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GPR119
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Metabolic Disease
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PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders .
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- HY-10435A
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(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide
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Dopamine Receptor
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Neurological Disease
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SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
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- HY-107384
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EMD-61753
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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- HY-B0007S
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GABA Receptor
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Neurological Disease
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Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
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- HY-10061
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AZD-3355
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GABA Receptor
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Metabolic Disease
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Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-W010820
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- HY-102064
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5-HT Receptor
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Neurological Disease
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SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
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- HY-P1217
-
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Melanocortin Receptor
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Inflammation/Immunology
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[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis .
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![[D-Trp8]-γ-MSH](//file.medchemexpress.eu/product_pic/hy-p1217.gif)
- HY-107384A
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EMD-61753 hydrochloride
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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- HY-14301
-
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BI1744
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Adrenergic Receptor
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Inflammation/Immunology
Endocrinology
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Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis .
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- HY-14301A
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BI1744 hydrochloride
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Adrenergic Receptor
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Inflammation/Immunology
Endocrinology
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Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis .
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- HY-14495A
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EX-1314 free base
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GHSR
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Metabolic Disease
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BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .
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- HY-101292
-
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PPAR
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Metabolic Disease
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FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes .
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- HY-10061B
-
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AZD-3355 hydrochloride
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GABA Receptor
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Metabolic Disease
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Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-103110
-
ST1936
1 Publications Verification
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
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- HY-W011220
-
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ADD-3878; U-63287
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PPAR
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Cardiovascular Disease
Cancer
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Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells .
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- HY-12363
-
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Opioid Receptor
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Neurological Disease
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U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
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- HY-101202A
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(Rac)-NIH 10815
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Opioid Receptor
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Neurological Disease
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(Rac)-SNC80 is a racemate of SNC80 (HY-101202). SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
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- HY-107708
-
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iGluR
Sigma Receptor
Potassium Channel
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Neurological Disease
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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 .
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- HY-103212A
-
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B-HT 933 hydrochloride; Oxazoloazepin hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy .
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- HY-100256R
-
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RAR/RXR
Autophagy
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Inflammation/Immunology
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Trifarotene (Standard) is the analytical standard of Trifarotene. This product is intended for research and analytical applications. Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively .
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- HY-13956R
-
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
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- HY-A0168R
-
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Adenosine Receptor
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Cardiovascular Disease
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Regadenoson (Standard) is the analytical standard of Regadenoson. This product is intended for research and analytical applications. Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
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- HY-119820
-
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SR57746A free base
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5-HT Receptor
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Neurological Disease
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Xaliproden free base is an orally active and selective 5-HT1A receptor agonist. Xaliproden free base shows analgesic effect against acute tonic nociceptive pain and has neuroprotective effects. Xaliproden free base has an acute inhibitory effect on paclitaxel (HY-B0015)-induced mechanical allodynia by inhibiting the excessive response of primary afferent neurons .
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- HY-14856
-
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PD 0200390
|
GABA Receptor
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Neurological Disease
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Atagabalin (PD 0200390) is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the GABA receptor by binding to the α2δ subunit of the GABA receptor, thereby increasing the GABA mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders .
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- HY-14302S1
-
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GR33343X-d5
|
Isotope-Labeled Compounds
Adrenergic Receptor
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Endocrinology
|
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Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
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- HY-105634AR
-
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Progesterone Receptor
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Endocrinology
Cancer
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Nomegestrol acetate (Standard) is the analytical standard of Nomegestrol acetate. This product is intended for research and analytical applications. Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
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- HY-12463
-
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Adrenergic Receptor
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Inflammation/Immunology
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Carmoterol hydrochloride is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors. Carmoterol hydrochloride can be used for the research of asthma and chronic obstructive pulmonary disease (COPD) .
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- HY-114076
-
|
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Others
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Neurological Disease
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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 .
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- HY-106278A
-
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PPAR
Others
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Metabolic Disease
|
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GW 590735 sodium is a potent and selective PPARα agonist with activity in regulating lipid metabolism. GW 590735 significantly increased high-density lipoprotein (HDL) cholesterol, decreased low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL) cholesterol, and significantly reduced triglycerides. The maximum increases in HDL cholesterol for GW 590735 were 37%, 53% and 84%, respectively, compared with bezafibrate, torcetrapib and GW 590735 .
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- HY-101514
-
-
- HY-17355
-
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Dopamine Receptor
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Neurological Disease
|
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Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
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- HY-B0410
-
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Dopamine Receptor
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Neurological Disease
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Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
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- HY-15565
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APD668
1 Publications Verification
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GPR119
Cytochrome P450
Potassium Channel
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Metabolic Disease
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APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
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- HY-14350
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Protease Activated Receptor (PAR)
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Others
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AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo .
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- HY-B0976AS
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Adrenergic Receptor
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Inflammation/Immunology
Endocrinology
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Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
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- HY-19835
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Free Fatty Acid Receptor
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Metabolic Disease
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LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM) .
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- HY-N0361
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- HY-P1019A
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction .
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![[Ala1,3,11,15]-Endothelin (53-63) (TFA)](//file.medchemexpress.eu/product_pic/hy-p1019a.gif)
- HY-120327
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KY-226
1 Publications Verification
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Phosphatase
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Neurological Disease
Metabolic Disease
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KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
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- HY-116771A
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Adrenergic Receptor
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Metabolic Disease
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CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors .CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate . CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-136390
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Dopamine Receptor
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Neurological Disease
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ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons .
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- HY-P1135
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Neuropeptide Y Receptor
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Neurological Disease
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M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin .
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- HY-P1163
-
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Vasopressin Receptor
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Cardiovascular Disease
Neurological Disease
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D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities .
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![D[LEU4,LYS8]-VP](//file.medchemexpress.eu/product_pic/hy-p1163.gif)
- HY-P1208
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Melanocortin Receptor
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Inflammation/Immunology
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PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo .
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- HY-P1217A
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Melanocortin Receptor
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Inflammation/Immunology
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[D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis .
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![[D-Trp8]-γ-MSH TFA](//file.medchemexpress.eu/product_pic/hy-p1217a.gif)
- HY-B0410A
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Dopamine Receptor
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Neurological Disease
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Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
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- HY-18679
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mGluR
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Neurological Disease
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TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
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- HY-103110A
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
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- HY-59201A
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nAChR
5-HT Receptor
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Neurological Disease
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A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
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- HY-10061A
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AZD-3355 napadisylate
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GABA Receptor
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Metabolic Disease
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Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-14803S
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BMS-214778-d5; VEC-162-d5
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Isotope-Labeled Compounds
Melatonin Receptor
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Neurological Disease
Endocrinology
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Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
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- HY-19884B
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RM-131 TFA; BIM-28131 TFA
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GHSR
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Metabolic Disease
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Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
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- HY-A0014S
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TAK-375-d5
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Isotope-Labeled Compounds
Melatonin Receptor
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Neurological Disease
Endocrinology
Cancer
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Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
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- HY-N2466A
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MT-I acetate; [Nle4,D-Phe7]-α-MSH acetate
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Melanocortin Receptor
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Cancer
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Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research .
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- HY-14539
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HF 1854
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Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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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) .
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- HY-153114
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FXR
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Inflammation/Immunology
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HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
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- HY-P1016B
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Endothelin Receptor
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Cardiovascular Disease
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BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
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- HY-125641
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5-HT Receptor
Adrenergic Receptor
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Cardiovascular Disease
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AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent .
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- HY-117167
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Thyroid Hormone Receptor
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Cancer
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KB-141 is a potent and selective TRβ agonist. The IC50 values are 23.9 nM and 3.3 nM for binding affinities from displacement of T3 from hTRα1 and hTRβ1, respectively. KB-141 has anti-obesity, anti-diabetic, and lipid-lowering effects?and can be used as an anti-cholesteremic agent in vivo .
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- HY-B0007R
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GABA Receptor
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Neurological Disease
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Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
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- HY-B0007S2
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GABA Receptor
Isotope-Labeled Compounds
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Neurological Disease
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Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
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- HY-17416R
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Guanfacine (hydrochloride) (Standard) is the analytical standard of Guanfacine (hydrochloride). This product is intended for research and analytical applications. Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-B0084R
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Progesterone Receptor
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Endocrinology
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Dienogest (Standard) is the analytical standard of Dienogest. This product is intended for research and analytical applications. Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
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- HY-14539A
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HF 1854 hydrochloride
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Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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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) .
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- HY-116771
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Adrenergic Receptor
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Metabolic Disease
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CL316243 free acid is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors. CL316243 free acid is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 free acid has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-101208
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- HY-P10716
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GLP Receptor
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Metabolic Disease
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Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
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- HY-119333
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mAChR
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Neurological Disease
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NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
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- HY-12463A
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Adrenergic Receptor
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Inflammation/Immunology
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Carmoterol is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors . Carmoterol can be used for the research of asthma and chronic obstructive pulmonary disease (COPD) .
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- HY-148418
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Free Fatty Acid Receptor
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Metabolic Disease
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TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes . TUG-499 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-B1658A
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(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate
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5-HT Receptor
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Neurological Disease
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Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
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- HY-B1658B
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(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
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5-HT Receptor
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Neurological Disease
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Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
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- HY-17453S
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GR 33343X-d3 xinafoate
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Isotope-Labeled Compounds
Adrenergic Receptor
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Inflammation/Immunology
Endocrinology
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Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
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- HY-126252
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ROR
Interleukin Related
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Inflammation/Immunology
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A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation .
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- HY-107489
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GABA Receptor
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Neurological Disease
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RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
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- HY-125996
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FXR
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Inflammation/Immunology
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NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease .
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- HY-128656
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Histamine Receptor
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Neurological Disease
Endocrinology
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LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
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- HY-118250
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Toll-like Receptor (TLR)
IFNAR
TNF Receptor
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Inflammation/Immunology
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GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma .
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- HY-P1135A
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Neuropeptide Y Receptor
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Neurological Disease
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M1145 TFA, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 TFA shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 TFA has an additive effect on the signal transduction of galanin .
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- HY-119486A
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(Rac)-PF-06649751; (Rac)-CVL-751
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Dopamine Receptor
Arrestin
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Neurological Disease
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(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
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- HY-P1163A
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Vasopressin Receptor
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Cardiovascular Disease
Neurological Disease
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D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities .
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![D[LEU4,LYS8]-VP TFA](//file.medchemexpress.eu/product_pic/hy-p1163a.gif)
- HY-21994
-
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5-HT Receptor
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Neurological Disease
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Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model .
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- HY-P2543
-
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Neuropeptide Y Receptor
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Metabolic Disease
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Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor .
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- HY-135483A
-
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nAChR
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Neurological Disease
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AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
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- HY-B0601
-
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AFP-172
|
Prostaglandin Receptor
Drug Metabolite
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
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Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma .
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- HY-17453S1
-
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GR 33343X-13C6 xinafoate
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
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Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
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- HY-A0039S1
-
|
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5-HT Receptor
|
Inflammation/Immunology
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Eletriptan-d5 is the deuterium labeled Eletriptan[1]. Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine[2].
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- HY-162423
-
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5-HT Receptor
Androgen Receptor
|
Neurological Disease
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CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .
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- HY-A0014R
-
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Melatonin Receptor
|
Neurological Disease
Endocrinology
Cancer
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|
Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
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-
- HY-W755295R
-
|
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Adrenergic Receptor
|
Cardiovascular Disease
|
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Mabuterol (hydrochloride) (Standard) is the analytical standard of Mabuterol (hydrochloride). This product is intended for research and analytical applications. Mabuterol hydrochloride is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol hydrochloride inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol hydrochloride suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB .
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- HY-118317
-
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Others
|
Cardiovascular Disease
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Zacopride is a selective agonist with the activity of enhancing the inward rectifier potassium current (IK1) in rabbit hearts. Zacopride also exhibits significant antiarrhythmic effects, inhibiting ventricular arrhythmias by increasing IK1 without affecting atrial arrhythmias. Zacopride can hyperpolarize the resting membrane potential and shorten the action potential duration (APD) in a concentration-dependent manner. Zacopride significantly reduced the incidence of compound-induced early afterdepolarizations (EADs) at 1 μmol/L .
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- HY-122211
-
|
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Others
|
Cardiovascular Disease
|
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MRS2802 is a P2Y14 receptor agonist with an EC50 value of 63 nM. MRS2802 can effectively activate the P2Y14 receptor and may play a role in regulating platelet function. The selectivity and activity of MRS2802 are conducive to in-depth research on the biological functions and pharmacological properties of P2Y receptors. The development of MRS2802 provides a potential inhibitory strategy for the search for new antiplatelet compounds .
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- HY-123389
-
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(R)-UM-1071
|
Others
|
Endocrinology
|
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MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .
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- HY-118250A
-
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Toll-like Receptor (TLR)
IFNAR
TNF Receptor
|
Inflammation/Immunology
|
|
GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma .
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- HY-P1320
-
|
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Opioid Receptor
|
Inflammation/Immunology
|
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[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
-
|
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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-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 .
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-
- HY-N2466
-
|
MT-I; [Nle4,D-Phe7]-α-MSH
|
Melanocortin Receptor
|
Neurological Disease
Cancer
|
|
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction .
|
-
- HY-110322A
-
|
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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-136576
-
|
|
LPL Receptor
Drug Metabolite
|
Inflammation/Immunology
|
|
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile .
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-
- HY-17386S
-
-
- HY-17356S
-
-
- HY-125881
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile .
|
-
- HY-W008947
-
|
|
LPL Receptor
ERK
Akt
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .
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-
- HY-135581
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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-
- HY-135582
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-P1208A
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo .
|
-
- HY-19411
-
|
|
nAChR
|
Neurological Disease
|
|
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus .
|
-
- HY-136233
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-101939
-
|
|
LPL Receptor
|
Neurological Disease
|
|
RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
|
-
- HY-101939A
-
|
|
LPL Receptor
|
Neurological Disease
|
|
RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
|
-
- 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-10457A
-
|
TD-5108 hydrochloride
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
- HY-108462
-
ML-SA1
3 Publications Verification
|
Dengue virus
TRP Channel
Flavivirus
|
Infection
|
|
ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral .
|
-
- HY-10457
-
|
TD-5108
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
- HY-120124
-
|
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
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-
- HY-103151
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP94253 hydrochloride is a potent and selective agonist of 5-HT1B receptor (Ki= 2 nM in a radioligand binding assay).Ki values for 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors are 89, 49, 860, and 1600 nM respectively . CP94253 hydrochloride is centrally active upon systemic administration in vivo .
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-
- HY-103512
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
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-
- HY-146332
-
|
|
Others
|
Cardiovascular Disease
|
|
Collagen-IN-1 (compound 3), an ortho-carbonyl hydroquinone derivative, is a selective inhibitor on collagen. Collagen-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner with an IC50 value of 1.77 μM. Collagen-IN-1 reduces the expression of P-selectin, activation of glycoprotein IIb/IIIa, and release of adenosine triphosphate and CD63 from platelet. Collagen-IN-1 has the potential for platelet-related thrombosis diseases research .
|
-
- HY-147660
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research .
|
-
- HY-19490
-
|
AQW-051
|
nAChR
|
Neurological Disease
|
|
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety .
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-
- HY-P4146
-
|
BI 456906
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
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-
- HY-17416AS
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Guanfacine- 13C, 15N3 is the 13C and 15N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].
|
-
- HY-A0039S2
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Eletriptan-d5 (hydrochloride) is the deuterium labeled Eletriptan hydrochloride[1]. Eletriptan (UK-116044) hydrochloride is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan hydrochloride has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan hydrochloride can be used for researching migraine[2].
|
-
- HY-107655
-
|
ABET
|
mAChR
|
Cardiovascular Disease
|
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research . Arecaidine but-2-ynyl ester (tosylate) 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-136233A
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-P3877A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(Leu31,Pro34)-Peptide YY (human) (TFA) is the TFA form of (Leu31,Pro34)-Peptide YY (human) (HY-P3877). (Leu31,Pro34)-Peptide YY (human) (TFA) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM .
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-
- HY-17416S2
-
|
|
Adrenergic Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
Endocrinology
|
|
Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
|
-
- HY-157940
-
|
|
Endothelin Receptor
|
Infection
|
|
Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC50 of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC50 of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism .
|
-
- HY-17416AS1
-
|
|
Adrenergic Receptor
Isotope-Labeled Compounds
|
Neurological Disease
Endocrinology
|
|
Guanfacine- 15N3, 13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
|
-
- HY-14171R
-
|
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
|
-
- HY-14803R
-
|
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
|
Tasimelteon (Standard) is the analytical standard of Tasimelteon. This product is intended for research and analytical applications. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
|
-
- HY-137370
-
|
HENECA; 2-Hexynyl-NECA
|
Adenosine Receptor
Amyloid-β
|
Neurological Disease
|
|
2-Hexynyl-5′-N-ethylcarboxamidoadenosine (HENECA) is a selective A2A adenosine receptor agonist. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine increases intracellular cAMP level, and inhibits TNFα-evoked MMP-3 release. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine induces Aβ42 production in SH-SY5Y cells .
|
-
- HY-17453R
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Salmeterol (xinafoate) (Standard) is the analytical standard of Salmeterol (xinafoate). This product is intended for research and analytical applications. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
|
-
- HY-120688
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
L-772405 is a selective 5-HT1D receptor agonist with the Ki values of 318, 29 and ＞ 1000 nM aganist guinea pig 5-HT1B receptor, guinea pig 5-HT1D receptor and rat 5-HT rransporter, respectively. L-772405 decreases the potassium-induced outflow of 5-HT with an IC50 value of 240 nM .
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-
- HY-10232S
-
|
Gaboxadol-d4
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
|
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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-
- HY-113756AR
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid (Standard) is the analytical standard of Latanoprost acid. This product is intended for research and analytical applications. Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor . Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes .
|
-
- HY-116149
-
|
|
Others
|
Others
|
|
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
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-
- HY-W116433
-
|
|
Others
|
Neurological Disease
|
|
SK609 is a selective dopamine D3 receptor agonist with activity that improves dopamine and norepinephrine levels in the cerebral cortex. SK609 has been successfully used to suppress dyskinesias in Parkinson's disease models and alleviated muscle twitches induced by L-dopa. SK609 improved performance in sustained attention tasks by significantly reducing misses and false alarms. SK609 may provide an inhibitory option for suppressing movement and cognitive impairment in patients with Parkinson's disease .
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-
- HY-115861
-
|
|
Others
|
Neurological Disease
|
|
UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies .
|
-
- 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-109114A
-
|
MT-7117 phosphate
|
Melanocortin Receptor
|
Metabolic Disease
|
|
Dersimelagon phosphate is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon phosphate shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation .
|
-
- HY-B1658BS
-
|
(R)-Frovatriptan-d3 succinate; SB 209509-d3 succinate; VML 251-d3 succinate
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
|
-
- HY-B1658AR
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan (succinate hydrate) (Standard) is the analytical standard of Frovatriptan (succinate hydrate). This product is intended for research and analytical applications. Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
|
-
- 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-14221
-
|
Lu 28-179
|
Sigma Receptor
|
Cancer
|
|
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
|
-
- HY-14221A
-
|
Lu 28-179 hydrochloride
|
Sigma Receptor
Ferroptosis
|
Cancer
|
|
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
|
-
- 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-17355S
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d7 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-119706
-
|
|
Apoptosis
Arrestin
|
Others
|
|
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .
|
-
- HY-113962
-
|
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
|
-
- HY-103138A
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .
|
-
- HY-118743
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors . KMN-80 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-100953
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research .
|
-
- HY-16729A
-
|
YKP10811 hydrochloride
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
|
-
- 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-109114
-
|
MT-7117
|
Melanocortin Receptor
|
Metabolic Disease
|
|
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation .
|
-
- HY-108020
-
|
|
Free Fatty Acid Receptor
|
Endocrinology
|
|
LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus . LY2881835 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-P1626
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
|
-
- HY-17355S1
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-17356S1
-
|
|
PPAR
Autophagy
Cytochrome P450
|
Cardiovascular Disease
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
|
-
- HY-B0410S1
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
- HY-103138
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
|
-
- HY-N0361S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
|
-
- HY-P4146A
-
|
BI 456906 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
|
-
- HY-17356R
-
|
|
PPAR
Cytochrome P450
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-14221B
-
|
LU-28-179 fumarate
|
Sigma Receptor
|
Cancer
|
|
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
|
-
- HY-121833
-
|
|
Trk Receptor
Akt
ERK
|
Neurological Disease
Cancer
|
|
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke .
|
-
- 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-118830
-
|
DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2
|
Prostaglandin Receptor
|
Endocrinology
|
|
13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
|
-
- HY-14301AR
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Olodaterol (hydrochloride) (Standard) is the analytical standard of Olodaterol (hydrochloride). This product is intended for research and analytical applications. Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis .
|
-
- HY-B0410R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole (Standard) is the analytical standard of Pramipexole. This product is intended for research and analytical applications. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-19057
-
|
MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
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 .
|
-
- HY-163712
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
|
-
- HY-17356S2
-
-
- HY-18100AR
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 (hydrochloride) (Standard) is the analytical standard of PRE-084 (hydrochloride). This product is intended for research and analytical applications. PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-N0361R
-
|
|
TRP Channel
Reactive Oxygen Species
Apoptosis
Caspase
Bcl-2 Family
Akt
PI3K
|
Cardiovascular Disease
Neurological Disease
|
|
Dihydrocapsaicin (Standard) is the analytical standard of Dihydrocapsaicin. This product is intended for research and analytical applications. Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
|
-
- HY-B0410AR
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole (dihydrochloride hydrate) (Standard) is the analytical standard of Pramipexole (dihydrochloride hydrate). This product is intended for research and analytical applications. Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-118944
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
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 .
|
-
- HY-103455
-
|
|
Others
|
Others
|
|
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
|
-
- HY-123426
-
|
|
GABA Receptor
|
|
|
JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors .
|
-
- HY-120045A
-
|
|
Others
|
Neurological Disease
|
|
DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .
|
-
- 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-108495
-
|
ML248
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .
|
-
- HY-16622A
-
|
|
LPL Receptor
|
Others
|
|
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
|
-
- HY-106993
-
|
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
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.
|
-
- HY-P0172A
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
-
- HY-N2037
-
|
Norcoclaurine; Demethyl-Coclaurine
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. 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 .
|
-
- HY-108494
-
|
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R .
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-
- HY-110353
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS .
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-
- HY-118152
-
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5-HT Receptor
|
Neurological Disease
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|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
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-
- HY-14363
-
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Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 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-100991
-
|
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
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-
- HY-16940
-
|
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
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-
- HY-P0172
-
|
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CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
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-
- HY-130344
-
|
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
|
SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression .
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-
- 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.
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-
- HY-122608
-
|
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
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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.
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-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
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-
- HY-P2847
-
|
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CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca 2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow .
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-
- HY-17355S2
-
|
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Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
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-
- HY-P4685
-
|
|
Angiotensin Receptor
|
Metabolic Disease
|
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
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-
- HY-10569S
-
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ACT-128800-d4
|
Isotope-Labeled Compounds
LPL Receptor
|
Others
|
|
Ponesimod-d4 (ACT-128800-d4)is the deuterium labeledPonesimod(HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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-
- HY-117356A
-
|
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P2Y Receptor
NF-κB
ERK
Apoptosis
|
Inflammation/Immunology
|
|
MRS2693 ammonium is the ammonium dalt form of MRS2693 (HY-117356). MRS2693 ammonium is a selective agonist for P2Y6 with an EC50 of 0.015 μM. MRS2693 ammonium protects C2C12 skeletal muscle cells from TNFα-induced apoptosis. MRS2693 ammonium reduces the activation of NF-kB, activates the ERK1/2 pathway, and has a cytoprotective effect on mouse ischemia-reperfusion injury model [2].
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-
- HY-15388S1
-
|
AGN 190168-13C2,d2
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
Cancer
|
|
Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene 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-W650803
-
|
A-57219
|
Others
|
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-124283
-
|
|
Others
|
Inflammation/Immunology
|
|
LEI-101 free base is a selective and orally bioavailable CB2 receptor agonist with the potential to inhibit diseases associated with inflammation and/or oxidative stress. LEI-101 free base has a binding potency to CB2 receptors that is approximately 100 times higher than that to CB1 receptors. Its pEC50 value on CB2 receptors is 8, while its pKi value on hERG is less than 4. LEI-101 may have an inhibitory effect on conditions such as kidney disease .
|
-
- HY-14915
-
|
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Others
|
Endocrinology
|
|
Bedoradrine is a highly selective β2-adrenergic agonist with activity in suppressing asthma and chronic obstructive pulmonary disease (COPD). Bedoradrine is administered by intravenous infusion and is specifically indicated for the suppression of acute asthma attacks. Bedoradrine has shown good safety and preliminary efficacy in clinical trials, especially in patients with stable moderate to severe asthma. The results of Bedoradrine studies have shown that it can provide clinical benefits without increasing clinical risks, especially for patients who are unable to use inhalation or nebulization suppression .
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-
- HY-14977
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
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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 .
|
-
- HY-15543A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
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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 .
|
-
- HY-14151
-
|
|
5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-19995
-
|
GSK 137647
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response .
|
-
- HY-15543
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
|
-
- HY-P1324
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake .
|
-
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide](//file.medchemexpress.eu/product_pic/hy-p1324.gif)
- HY-P1324A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake .
|
-
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA](//file.medchemexpress.eu/product_pic/hy-p1324a.gif)
- HY-103412
-
|
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
|
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression .
|
-
- HY-116522
-
-
- HY-110291
-
|
|
Others
|
Neurological Disease
|
|
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .
|
-
- 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.
|
-
- HY-108501
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
(1R,1'S,3'R/1R,1'R,3'S)-L-054,264 is a selective non-peptide human somatostatin receptor subtype 2 (sst2) agonist. (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 can be used in the study of retinal neuromodulation .
|
-
- HY-17356G
-
|
|
Cytochrome P450
PPAR
Autophagy
|
Cardiovascular Disease
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-14152
-
|
|
5-HT Receptor
|
Cancer
|
|
Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- 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 .
|
-
- HY-162712
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX-201 is a selective agonist for OX2R with an EC50 of 8 nM. Pathological proteins produced by neurons are released into the interstitial fluid (ISF) in a manner dependent on neuronal activity and are cleared from the brain via lymphatic pathways. The outflow of pathological proteins to the ISF is related to the arousal state of neurons. OX-201 can induce neuronal awakening and promote the release of tau into the hippocampal ISF. Although OX-201 does not alter hippocampal tau levels, it has potential applications for Alzheimer's disease (AD) associated with sleep/wake rhythm disturbances .
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-
- HY-120144
-
|
|
Others
|
Neurological Disease
|
|
SR-8993 is a highly selective nociceptin receptor agonist that can penetrate the blood-brain barrier and has the activity of reducing alcohol intake and relieving withdrawal anxiety. SR-8993 has shown mild anxiolytic effects in animal models and can effectively reverse anxiety caused by acute alcohol withdrawal. SR-8993 further reduces restricted drinking, operant responses for alcohol, and increased drinking induced by long-term intermittent exposure to alcohol. SR-8993 also reduces stress- and cue-related alcohol-seeking relapse .
|
-
- 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-12694
-
|
R-108512
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
|
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-12946A
-
|
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- HY-100839
-
|
D,L-(tetrazol-5-yl)glycine; LY 285265
|
iGluR
|
Neurological Disease
|
|
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist . (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively . (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice .
|
-
- HY-12946
-
|
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- 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-117734
-
|
|
iGluR
|
Neurological Disease
|
|
PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors .
|
-
- HY-135581S1
-
|
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Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
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- HY-135582S1
-
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
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Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
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- HY-10569S1
-
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ACT-128800-d7
|
Isotope-Labeled Compounds
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Others
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|
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-135582S
-
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Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-129922
-
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Prostaglandin Receptor
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Endocrinology
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Prostaglandin I2 is an unstable prostanoid which, through the ‘I prostanoid’ (IP) receptor, inhibits platelet aggregation and promotes vasodilatation in pulmonary vascular beds. AFP 07 is a 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki=0.561 nM).1 AFP 07 shows weaker affinity for EP receptors, with Ki values > 100 nM for EP1-3 and > 10 nM for EP4. 16(R)-AFP 07 is an epimer of AFP 07. Its biological properties, particularly through the IP and EP receptors, remain to be evaluated.
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- HY-15746
-
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
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Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
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- HY-17038S1
-
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S-20098-d4
|
Isotope-Labeled Compounds
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
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Neurological Disease
|
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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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S-20098-d3
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
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Agomelatin-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-10968A
-
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LPL Receptor
|
Neurological Disease
|
|
CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS) .
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- HY-108568
-
|
15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
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|
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
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- HY-108511A
-
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Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
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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 .
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- HY-W009009
-
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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 .
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-
- HY-10968
-
CYM5442
1 Publications Verification
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LPL Receptor
|
Neurological Disease
|
|
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .
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- HY-108511
-
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Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
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|
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 .
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- HY-15746A
-
|
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
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Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion .
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- 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 .
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- HY-17038R
-
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Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
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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 .
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-
- HY-19927A
-
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5-HT Receptor
|
Neurological Disease
Endocrinology
|
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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 .
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- HY-W052508
-
|
N-Desalkylquetiapine
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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 .
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- HY-B0084S4
-
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STS 557-13C,15N,d4
|
Isotope-Labeled Compounds
Progesterone Receptor
|
Endocrinology
|
|
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
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- HY-19545A
-
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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 .
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- HY-10624
-
THIQ
1 Publications Verification
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Melanocortin Receptor
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Metabolic Disease
|
|
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
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- HY-108400
-
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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 .
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-
- HY-138879B
-
|
(1S,5R)-CP-601927
|
nAChR
|
Neurological Disease
|
|
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
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-
- HY-100554
-
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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 .
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- HY-15746B
-
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion .
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-
- HY-P3849
-
|
LMN-NKA
|
Neurokinin Receptor
|
Neurological Disease
|
|
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
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-
![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](//file.medchemexpress.eu/product_pic/hy-p3849.gif)
- HY-19842
-
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CVT 3619
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
GS-9667 (CVT 3619), a novel N 6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .
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- HY-14151R
-
|
|
5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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-
- HY-103151A
-
|
|
5-HT Receptor
|
Others
|
|
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. CP94253 binds to the 5-HT1B, 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors, with Kis of 2, 89, 49, 860 and 1600 nM. CP94253 causes satiety, anorexia, weight loss and hyperlocomotion in rats model .
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-
- HY-101341
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
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- HY-103216A
-
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Adrenergic Receptor
|
Neurological Disease
|
|
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
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-
- HY-160959
-
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nAChR
|
Neurological Disease
|
|
AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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- HY-121129
-
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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 .
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-
- HY-124110
-
|
|
nAChR
|
Neurological Disease
|
|
TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ∗ and α4β2 ∗ nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ∗ nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ∗ nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
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-
- HY-15997
-
|
(-)-Trans-(1S,2S)-U-50488 hydrochloride
|
Opioid Receptor
|
Infection
Cancer
|
|
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
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-
- HY-168168
-
|
|
Others
|
Metabolic Disease
|
|
(5aS,6R,6aR)-MK-8666 is a selective GPR40 agonist with activity in promoting fatty acid-induced insulin secretion in pancreatic β cells and intestinal enteroendocrine cells. (5aS,6R,6aR)-MK-8666 has been studied for the inhibition of type 2 diabetes and has shown significant blood glucose lowering effects. Although (5aS,6R,6aR)-MK-8666 is considered to have potential inhibitory advantages, its development was stopped in Phase I clinical trials due to liver safety issues .
|
-
- HY-100370
-
|
|
GABA Receptor
|
Cancer
|
|
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
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-
- HY-15746S1
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
(rac)-Dobutamine-d6 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
|
-
- HY-15746S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
(rac)-Dobutamine-d4 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
|
-
- HY-103120
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor .
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-
- HY-155811
-
|
|
Others
|
Neurological Disease
|
|
DQP-997-74 (compound 2i) is a selective inhibitor of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
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- HY-15746R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Dobutamine (hydrochloride) (Standard) is the analytical standard of Dobutamine (hydrochloride). This product is intended for research and analytical applications. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
|
-
- HY-108663
-
|
5-Methoxyuridine 5'-trihydrogen diphosphate
|
P2Y Receptor
|
Neurological Disease
Metabolic Disease
|
|
5-OMe-UDP (5-methoxyuridine 5'-trihydrogen diphosphate) is a P2Y6 receptor agonist (EC50=0.08 μM). 5-OMe-UDP activates the P2Y6 receptor by binding to it, which triggers signaling pathways within the cell. This activation can lead to an increase in intracellular calcium ion concentration, which in turn regulates cellular function. The methoxy groups of 5-OMe-UDP provide additional activity and selectivity, contributing to the binding of 5-OMe-UDP to the P2Y6 receptor. 5-OMe-UDP can be used to study diseases related to P2Y6 receptor function, such as diabetes, inflammatory bowel disease, Alzheimer's disease, etc .
|
-
- 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-108568S
-
|
15d-PGJ2-d4; 15-Deoxy-Δ12,14-PGJ2-d4
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
|
-
- HY-108568R
-
|
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
15-Deoxy-Δ-12,14-prostaglandin J2 (Standard) is the analytical standard of 15-Deoxy-Δ-12,14-prostaglandin J2. This product is intended for research and analytical applications. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 μM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
|
-
- 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.
|
-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
- HY-151738
-
|
|
ADC Linker
|
Others
|
|
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-125782
-
|
15(R)-15-Methyl PGD2
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
15(R)-15-Methyl prostaglandin D2 (15(R)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1and CRTH2/DP2. 15(R)-15-Methyl prostaglandin D2 is a potent, selective agonist for the CRTH2/DP2 receptor. The EC50 values for eosinophil CD11b expression, actin polymerization, and chemotaxis are 1.4, 3.8, and 1.7 nM, respectively, each of which is approximately 3-5 fold lower than those for PGD2. In contrast the EC50 for the DP1-mediated increase in platelet cAMP by 15(R)-15-methyl PGD2 is >10 μM.
|
-
- HY-135763
-
|
Met-36
|
Others
|
Others
|
|
Metabolex-36 is a FFA4 agonist developed by Metabolex (now Cymabay Therapeutics) and used in multiple studies to investigate the function of FFA4. Metabolex-36 was used in conjunction with AstraZeneca compounds (AZ-423 and AZ-670) to investigate FFA4 function in pancreatic delta cells. Metabolex-36 has a pEC50 of 5.9 for FFA4 and a pEC50 of less than 4.0 for FFA1. Compound B was used to investigate the role of FFA4 in growth hormone-releasing peptide (ghrelin) secretion and somatostatin release and was used with FFA4 KO mice. Compound B had an EC50 of 15 nM for FFA4 in an IP3 accumulation assay in FFA4-transfected COS7 cells and was up to 1000-fold selective for FFA1. Compound B inhibited baseline ghrelin secretion from primary gastric mucosal cells but had no effect on cells from FFA4 KO mice. Oral administration of Compound B reduced plasma ghrelin levels in mice under starvation conditions. Compound B also inhibited somatostatin release from primary gastric epithelial cells but had no effect on cells from FFA4 KO mice.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-10475G
-
|
CD336 (GMP); NSC608001 (GMP); Ro 40-6055 (GMP)
|
Fluorescent Dye
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
|
-
- HY-111582G
-
|
|
Fluorescent Dye
|
|
BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .
|
-
- HY-17356G
-
|
|
Fluorescent Dye
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
| Cat. No. |
Product Name |
Type |
-
- HY-10475G
-
|
CD336 (GMP); NSC608001 (GMP); Ro 40-6055 (GMP)
|
Biochemical Assay Reagents
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
|
-
- HY-111582G
-
|
|
Biochemical Assay Reagents
|
|
BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .
|
-
- HY-17356G
-
|
|
Biochemical Assay Reagents
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-15401A
-
|
|
Biochemical Assay Reagents
|
|
WAY-163909 hydrochloride is a potent 5-hydroxytryptamine receptor 2C (5-HT2C) agonist with an EC50 of 8 nM and a maximum efficacy of 90%, while displaying minimal activity at 5-HT2A receptors. Its selectivity is further demonstrated by Ki values of 10.5 nM for 5-HT2C, alongside higher Ki values for 5-HT2A (212 nM), 5-HT7 (343 nM), and 5-HT2B (485 nM), and it lacks significant activity at various other receptors.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2518
-
|
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
|
-
- HY-P2518A
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
|
-
- HY-P1336
-
-
- HY-P1013A
-
-
- HY-P1480
-
-
- HY-P0226A
-
-
- HY-P1013
-
-
- HY-P0226
-
-
- HY-P1011
-
-
- HY-16465
-
-
- HY-P1738
-
-
- HY-P1334
-
-
- HY-P2572
-
-
- HY-P1334A
-
-
- HY-136623
-
-
- HY-P1033
-
-
- HY-16465A
-
-
- HY-P10639
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR2 agonist P32 (Ac-RHYPYWR-OH) is a C5aR2-selective agonist. C5aR2 agonist P32 has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo .
|
-
- HY-145237
-
BM213
1 Publications Verification
|
Peptides
|
Cancer
|
|
BM213, a potent and selective agonist for C5aR1, shows antitumor activity in a mouse model of mammary carcinoma.
|
-
- HY-P2018
-
-
- HY-P3876
-
-
- HY-P1588
-
-
- HY-P0210
-
DAMGO
4 Publications Verification
|
Opioid Receptor
|
Cancer
|
|
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-P0177
-
-
- HY-P3870
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
|
-
- HY-P3870A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
|
-
- HY-P1198
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
|
-
- HY-17584
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-P1012
-
-
- HY-P0210B
-
|
|
Opioid Receptor
|
Cancer
|
|
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-105239A
-
|
FE 202158 acetate
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Selepressin (FE 202158) acetate is a selective vasopressin V1A receptor agonist. Selepressin acetate is a potent vasopressin. Selepressin acetate can be used in the study of septic shock.
|
-
- HY-17584A
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide acetate is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-P0298
-
-
- HY-P0298A
-
-
- HY-P1012A
-
-
- HY-P2475
-
-
- HY-P3870B
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
|
-
- HY-P0078
-
TRAP-6
4 Publications Verification
PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4 .
|
-
- HY-P1198A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
|
-
- 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-P1314
-
-
- HY-P1030
-
|
|
Neurokinin Receptor
|
Endocrinology
|
|
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
|
-
- HY-105239
-
|
FE 202158
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Selepressin (FE 202158) is a selective vasopressin V1A receptor agonist. Selepressin is a potent vasopressor. Selepressin can be used in the research of septic shock .
|
-
- HY-P3851
-
-
- HY-P3030
-
|
|
Peptides
|
Inflammation/Immunology
|
|
CPN-219, a next-generation hexapeptidic NMUR2 agonist, achieves a dose-dependent and selective activation of NMUR2 with an EC50 value of 2.2 nM .
|
-
- HY-P1314A
-
-
- HY-P1160
-
|
|
GCGR
|
Metabolic Disease
|
|
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes .
|
-
- HY-P1341
-
|
Orexin A (17-33) (human, mouse, rat, bovine)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
|
-
- HY-P3684A
-
|
|
CRFR
|
Neurological Disease
|
|
[DPro5] Corticotropin Releasing Factor, human, rat TFA is a selective corticotropin releasing factor/hormone R2 (CRH-R2)agonist. [DPro5] Corticotropin Releasing Factor, human, rat TFA fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat .
|
-
- HY-P0186
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
|
- HY-P1341A
-
|
Orexin A (17-33) (human, mouse, rat, bovine) TFA
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
|
- HY-P5506
-
|
|
Complement System
|
Others
|
|
C5a Receptor agonist, W5Cha (Peptide 1) is a selective complement C5a receptor (C5aR) agonist (EC50=0.2 μM), a hexapeptide derived from the C-terminus of C5a with specific amino acid modifications. C5a Receptor agonist, W5Cha is able to interact with the Arg-206 site of the C5a receptor through its C-terminal arginine, thereby activating the receptor .
|
- HY-P1160A
-
|
|
GCGR
|
Metabolic Disease
|
|
Bay 55-9837 TFA is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 TFA may be a useful therapy for the research of type 2 diabetes .
|
- HY-P1752
-
|
|
CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II (human) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior .
|
- HY-P0186A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
|
- HY-P1752A
-
|
|
CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II, human (TFA) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior .
|
- HY-129271
-
|
Deltorphin A; Dermenkephalin
|
Opioid Receptor
|
Others
|
|
Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
|
- HY-105155
-
|
RMP 7
|
Bradykinin Receptor
|
Cancer
|
|
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
|
- HY-P3877
-
- HY-P3891
-
- HY-110366
-
|
SAX-187 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .
|
- HY-P1279
-
- HY-P1167
-
- HY-P2210
-
|
|
GPR171
|
Metabolic Disease
|
|
BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. BigLEN(mouse) can be used to regulate responses associated with food intake and metabolism .
|
- HY-P1279A
-
- HY-P3597
-
|
|
CFTR
|
Others
|
|
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with high affinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit .
|
- HY-P5358
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
|
- HY-P10291
-
- HY-17584R
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Linaclotide (Standard) is the analytical standard of Linaclotide. This product is intended for research and analytical applications. Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
- HY-P5172
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
|
- HY-P1295
-
|
Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
|
- HY-P1167A
-
- HY-P1332
-
|
[D-Ser2, Leu5, Thr6]-enkephalin
|
Opioid Receptor
|
Neurological Disease
|
|
DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor .
|
- HY-P1129
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
AR-M1896 is a GalR2 selective agonist with a binding IC50 of 1.76 nM for rat GalR2. AR-M1896 can be used for the research of acute myocardial infarction and neuropathic pain .
|
- HY-P1322
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats .
|
- HY-17609
-
|
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
- HY-P1132A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect .
|
- HY-P3462A
-
|
|
CGRP Receptor
|
Metabolic Disease
|
|
Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
|
- HY-P3609
-
|
JNJ 38488502; FE 200665
|
Opioid Receptor
|
Neurological Disease
|
|
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
|
- HY-P3134
-
|
|
Peptides
|
Metabolic Disease
|
|
CPN-267 (compound 7b) is a selective neuromedin U receptor 1 (NMUR1) agonist with the EC50 of 0.25 nM. CPN-267 suppresses body weight gain in mice and can be used for study of obesity .
|
- HY-P99004
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family .
|
- HY-P1390
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors .
|
- HY-P10579
-
|
|
Ephrin Receptor
|
Cancer
|
|
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
|
- HY-P1338
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
- HY-P4107
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr) .
|
- HY-P1325
-
|
((Cys31, Nva 34)-Neuropeptide Y (27-36))2
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BWX 46 (((Cys31, Nva 34)-Neuropeptide Y (27-36))2) is a selective Y5 receptor agonist with an IC50 value of 0.85 nM. BWX 46 can inhibit the synthesis of cAMP in Y5 cells .
|
- HY-P1322A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats .
|
- HY-P3124A
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly .
|
- HY-P3124
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly .
|
- HY-W344602
-
|
|
Peptides
|
Others
|
|
Substance P, [Met-OMet11] is a selective SP-P agonist. Substance P, [Met-OMet11] also is an active peptide. Substance P, [Met-OMet11] can be used for various biochemical studies .
|
- HY-P3958
-
|
|
Peptides
|
Neurological Disease
|
|
BIM-23027 is a selective agonist of sst2 receptor (EC50=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism .
|
- HY-P4678
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
(Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
|
- HY-P4678A
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
(Phe2,Orn8)-Oxytocin acetate is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin acetate induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM .
|
- HY-P1390A
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors .
|
- HY-P0185
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
- HY-P1338A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
- HY-P0185A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
- HY-153963
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
- HY-P1340
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
- HY-P1301
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
- HY-P3498
-
|
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
- HY-P0198B
-
- HY-P0208
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects .
|
- HY-P1340A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
- HY-P1300
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
- HY-P1301A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
- HY-P1810
-
|
|
Peptides
|
Neurological Disease
|
|
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively .
|
- HY-P1214
-
- HY-P1096
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
|
- HY-P2242A
-
|
|
Melanocortin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects .
|
- HY-P1112
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
- HY-P1316
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
|
- HY-P1316A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
|
- HY-P2454
-
|
|
Bacterial
|
Infection
|
|
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent .
|
- HY-P3057
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension .
|
- HY-P3433
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively .
|
- HY-P1214A
-
- HY-P1112A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
- HY-P3155
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R .
|
- HY-P1809
-
|
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2
|
Peptides
|
Metabolic Disease
|
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
- 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-P1809A
-
|
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2 acetate
|
Peptides
|
Metabolic Disease
|
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) acetate is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
- HY-103292
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
[Phe8Ψ(CH-NH)Arg9]-Bradykinin is a selective Bradykinin receptor B2 agonist (not cleaved by protein kinase I/II). [Phe8Ψ(CH-NH)Arg9]-Bradykinin has potential for the research of hypertension .
|
- HY-P1033S
-
- HY-P1206
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
|
- HY-P1117
-
|
|
Formyl Peptide Receptor (FPR)
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK1 potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity .
|
- HY-P5372
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
|
- HY-P1744
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
- HY-P1117A
-
|
|
Formyl Peptide Receptor (FPR)
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
MMK1 TFA is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 TFA is a potent chemotactic and calcium-mobilizing agonist. MMK1 TFA potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 TFA exerts anxiolytic-like activity .
|
- 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-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-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 .
|
- HY-153963A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
- HY-12554A
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
|
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
- HY-P1131A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 TFA is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617 TFA, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
- HY-P1397A
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
|
|
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
- HY-111615A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
- HY-19884
-
|
RM-131; BIM-28131
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
- HY-P3684
-
|
|
CRFR
|
Endocrinology
|
|
[DPro5] Corticotropin Releasing Factor, human, rat is a selective R2 agonist of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin. [DPro5] Corticotropin Releasing Factor, human, rat fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat .
|
- HY-103295
-
|
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors .
|
- HY-P1016
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 1 2.
|
- HY-P1368
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
|
- HY-12554B
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
- HY-P1033S1
-
- HY-P10336
-
|
|
Peptides
|
Neurological Disease
Endocrinology
|
|
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .
|
- HY-103295A
-
|
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors .
|
- HY-19884A
-
|
RM-131 acetate; BIM-28131 acetate
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
- HY-P1019
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction
|
- HY-P4195
-
|
|
Peptides
|
Metabolic Disease
|
|
[K15,R16,L27]VIP(1-7)/GRF(8-27), a VIP1 selective agonist, exhibits IC50 values of binding of 2 nM, 1 nM, 30,000 nM for the human VIP1, rat VIP1, rat VIP2 receptors, respectively . VIP: VASOACTIVE Intestinal Polypeptide
|
- HY-103291
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings .
|
- HY-P1368A
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
|
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
- HY-P1217
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis .
|
- HY-P1019A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction .
|
- HY-P1163
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities .
|
- HY-P1208
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo .
|
- HY-P1217A
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
[D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis .
|
- HY-19884B
-
|
RM-131 TFA; BIM-28131 TFA
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
- HY-N2466A
-
|
MT-I acetate; [Nle4,D-Phe7]-α-MSH acetate
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research .
|
- HY-P1016B
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
|
- HY-P10716
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
|
- HY-P1135A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
M1145 TFA, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 TFA shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 TFA has an additive effect on the signal transduction of galanin .
|
- HY-P1163A
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities .
|
- HY-P2543
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor .
|
- 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-N2466
-
|
MT-I; [Nle4,D-Phe7]-α-MSH
|
Melanocortin Receptor
|
Neurological Disease
Cancer
|
|
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction .
|
- HY-P1208A
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo .
|
- HY-P4146
-
|
BI 456906
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
|
- HY-P3877A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(Leu31,Pro34)-Peptide YY (human) (TFA) is the TFA form of (Leu31,Pro34)-Peptide YY (human) (HY-P3877). (Leu31,Pro34)-Peptide YY (human) (TFA) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM .
|
- HY-P1626
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
|
- HY-P4146A
-
|
BI 456906 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
|
- HY-P0172A
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
- HY-P0172
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
- HY-P2847
-
|
|
CRFR
|
Metabolic Disease
Endocrinology
|
|
Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca 2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow .
|
- HY-P4685
-
|
|
Angiotensin Receptor
|
Metabolic Disease
|
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
|
- HY-P1324
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake .
|
- HY-P1324A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake .
|
- 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-P3849
-
|
LMN-NKA
|
Neurokinin Receptor
|
Neurological Disease
|
|
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
|
- HY-P4195A
-
|
|
Peptides
|
Metabolic Disease
|
|
[K15,R16,L27]VIP(1-7)/GRF(8-27) (acetate) is the acetate of [K15,R16,L27]VIP(1-7)/GRF(8-27) (HY-P4195). [K15,R16,L27]VIP(1-7)/GRF(8-27) (acetate), a VIP1 selective agonist, exhibits IC50 values of binding of 2 nM, 1 nM, 30,000 nM for? the human VIP1, rat VIP1, rat VIP2 receptors, respectively . VIP: VASOACTIVE Intestinal Polypeptide
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99665
-
|
LY-3209590
|
Insulin Receptor
|
Metabolic Disease
|
|
Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
|
-
- 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 |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-79593S2
-
|
|
|
MRE-269-d7 is deuterium labeled MRE-269 (HY-79593). MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist[1][2].
|
-
-
- HY-103005S
-
|
|
|
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
|
-
-
- HY-B0197S
-
|
|
|
Naratriptan-d3 is the deuterium labeled Naratriptan[1]. Naratriptan is a selective 5-HT1 receptor subtype agonist[2].
|
-
-
- HY-105791S
-
|
|
|
Sulazepam-d5 is a deuterium labeled Sulazepam (HY-105791). Sulazepam is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist[1].
|
-
-
- HY-B0010S
-
|
|
|
Formoterol-d6 is the deuterium labeled Formoterol. Formoterol ((±)Formoterol) is a potent, selective and long-acting β2-adrenoceptor agonist[1].
|
-
-
- HY-14773S
-
|
|
|
(Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
|
-
-
- HY-B0189S1
-
|
|
|
Mosapride-d5 is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
|
-
-
- HY-B0197AS
-
|
|
|
Naratriptan-d3 (hydrochloride) is the deuterium labeled Naratriptan, which is a selective 5-HT1 receptor subtype agonist.
|
-
-
- HY-N6807S
-
|
|
|
Elemicin-d3 is deuterated labeled Pemafibrate (HY-17618). Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.
|
-
-
- HY-100532S
-
|
|
|
CD437- 13C6 is the 13C- and deuterium labeled CD437. CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
|
-
-
- HY-15388S
-
|
|
|
Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris[1][2].
|
-
-
- HY-79593S1
-
|
|
|
MRE-269-d6 is deuterium labeled MRE-269. MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
|
-
-
- HY-17416S
-
|
|
|
Guanfacine-d2 (hydrochloride) is the deuterium labeled Guanfacine hydrochloride. Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors .
|
-
-
- HY-B0374S1
-
|
|
|
Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
|
-
-
- HY-B0545S
-
|
|
|
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
|
-
-
- HY-14171S
-
|
|
|
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
|
-
-
- HY-B0374S
-
|
|
|
Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine. Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent[1][2].
|
-
-
- HY-B0374AS
-
|
|
|
Moxonidine- 13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) hydrochloride is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
|
-
-
- HY-B0383AS2
-
|
|
|
Almotriptan-d3 benzoate is deuterated labeled Almotriptan (HY-B0383A). Almotriptan is a selective agonist of 5-HT 1B/1D Receptor. Almotriptan can used in study of migraine attacks .
|
-
-
- HY-12199BS
-
|
|
|
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
|
-
-
- HY-12222S
-
|
|
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Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
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- HY-12222S1
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Obeticholic Acid-d4 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
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- HY-A0039S
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Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
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- HY-17034AS
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Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
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- HY-100490S
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Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
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- HY-13956S
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Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
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- HY-15831
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L-838417-d9 is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].
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- HY-B1052S
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Lofexidine-d4 (hydrochloride) (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride. Lofexidine hydrochloride is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
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- HY-17043S
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Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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- HY-B0471S
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Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-17043S1
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Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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- HY-B0154S
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Fluticasone propionate-d3 is the deuterium labeled Fluticasone propionate. Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].
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- HY-B0154S1
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Fluticasone propionate-d5 is deuterium labeled Fluticasone (propionate). Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].
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- HY-B0471S3
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Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0225AS
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Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system[1][2].
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- HY-B0471S2
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(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0180S
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Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
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- HY-B0180S1
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Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
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- HY-B0468S
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Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
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- HY-P1033S
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Pyr1]-Apelin-13, Gly(15N) TFA is a Gly 15N labeled [Pyr1]-Apelin-13. [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor agonist .
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- HY-B0471S1
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Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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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-A0168S
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Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
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- HY-13956S1
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Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
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- HY-17386S1
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Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .
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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-P1033S1
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[Pyr1]-Apelin-13, Pro( 13C5, 15N) (TFA) is the 13C and 15N labeled isotope of [Pyr1]-Apelin-13(HY-P1033).[Pyr1]-Apelin-13 is a potent and selective endogenous apelin receptor agonist .
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- HY-135392S
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N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
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- HY-135119
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Salmeterol-d3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
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- HY-113962S
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7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
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- HY-14262S1
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Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-B0007S
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Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
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- HY-14302S1
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Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
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- HY-B0976AS
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Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
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- HY-14803S
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Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
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- HY-A0014S
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Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
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- HY-B0007S2
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Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
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- HY-17453S
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Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
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- HY-17453S1
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Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
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- HY-A0039S1
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Eletriptan-d5 is the deuterium labeled Eletriptan[1]. Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine[2].
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- HY-17386S
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Rosiglitazone-d3 is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].
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- HY-17356S
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Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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- HY-17416AS
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Guanfacine- 13C, 15N3 is the 13C and 15N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].
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- HY-A0039S2
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Eletriptan-d5 (hydrochloride) is the deuterium labeled Eletriptan hydrochloride[1]. Eletriptan (UK-116044) hydrochloride is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan hydrochloride has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan hydrochloride can be used for researching migraine[2].
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- HY-17416S2
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Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-17416AS1
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Guanfacine- 15N3, 13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
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- HY-10232S
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THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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- HY-B1658BS
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Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
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- HY-17355S
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Pramipexole-d7 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
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- HY-17355S1
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Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
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- HY-17356S1
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Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
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- HY-B0410S1
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Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
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- HY-N0361S
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Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
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- HY-17356S2
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Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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- HY-17355S2
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Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
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- HY-10569S
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Ponesimod-d4 (ACT-128800-d4)is the deuterium labeledPonesimod(HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-15388S1
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Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene 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-135581S1
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Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
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- HY-135582S1
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Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
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- HY-10569S1
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Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-135582S
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Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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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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Agomelatin-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-B0084S4
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Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
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- HY-15746S1
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(rac)-Dobutamine-d6 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
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- HY-15746S
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(rac)-Dobutamine-d4 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
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- HY-108568S
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15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
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Classification |
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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-155480
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Alkynes
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PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC50s of 11.2 nM and 30.0 nM in Ca 2+ and β-arrestin experiments, respectively .
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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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- HY-107681
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Alkynes
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SIB-1508Y is an orally active and selective nAChR agonist. SIB-1508Y has the potential to study parkinsonism . SIB-1508Y 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-123249
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Alkynes
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HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 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-151738
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Azide
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Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-111582
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Adjuvant
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BBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of ?59.1?nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .
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![[Sar9] Substance P](http://file.medchemexpress.eu/product_pic/hy-p1738.gif)
![[Pyr1]-Apelin-13](http://file.medchemexpress.eu/product_pic/hy-p1033.gif)
![[Sar9,Met(O2)11]-Substance P](http://file.medchemexpress.eu/product_pic/hy-p1012.gif)
![[Des-Arg9]-Bradykinin](http://file.medchemexpress.eu/product_pic/hy-p0298.gif)
![[Des-Arg9]-Bradykinin acetate](http://file.medchemexpress.eu/product_pic/hy-p0298a.gif)
![[Sar9,Met(O2)11]-Substance P TFA](http://file.medchemexpress.eu/product_pic/hy-p1012a.gif)
![[Pro9]-Substance P](http://file.medchemexpress.eu/product_pic/hy-p2475.gif)
![[DPro5] Corticotropin Releasing Factor, human, rat TFA](http://file.medchemexpress.eu/product_pic/hy-p3684a.gif)
![[Lys5,MeLeu9,Nle10]-NKA(4-10)](http://file.medchemexpress.eu/product_pic/hy-p1279.gif)
![[Orn5]-URP](http://file.medchemexpress.eu/product_pic/hy-p1167.gif)
![[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA](http://file.medchemexpress.eu/product_pic/hy-p1279a.gif)
![[Pro34]Neuropeptide Y, porcine](http://file.medchemexpress.eu/product_pic/hy-p10291.gif)
![[Orn5]-URP TFA](http://file.medchemexpress.eu/product_pic/hy-p1167a.gif)
![[D-Trp34]-Neuropeptide Y](http://file.medchemexpress.eu/product_pic/hy-p1322.gif)
![d[Cha4]-AVP](http://file.medchemexpress.eu/product_pic/hy-p1390.gif)
![[D-Trp34]-Neuropeptide Y TFA](http://file.medchemexpress.eu/product_pic/hy-p1322a.gif)
![d[Cha4]-AVP TFA](http://file.medchemexpress.eu/product_pic/hy-p1390a.gif)
![[Ala11,D-Leu15]-Orexin B(human)](http://file.medchemexpress.eu/product_pic/hy-p1340.gif)
![[Arg14,Lys15]Nociceptin](http://file.medchemexpress.eu/product_pic/hy-p1301.gif)
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](http://file.medchemexpress.eu/product_pic/hy-p10148.gif)
![[D-Arg25]-Neuropeptide Y (human)](http://file.medchemexpress.eu/product_pic/hy-p0198b.gif)
![[Leu31,Pro34]-Neuropeptide Y (porcine)](http://file.medchemexpress.eu/product_pic/hy-p0208.gif)
![[Ala11,D-Leu15]-Orexin B(human) TFA](http://file.medchemexpress.eu/product_pic/hy-p1340a.gif)
![[(pF)Phe4]Nociceptin(1-13)NH2](http://file.medchemexpress.eu/product_pic/hy-p1300.gif)
![[Arg14,Lys15]Nociceptin TFA](http://file.medchemexpress.eu/product_pic/hy-p1301a.gif)
![[(pF)Phe4]Nociceptin(1-13)NH2 TFA](http://file.medchemexpress.eu/product_pic/hy-p1300a.gif)
![[D-Trp11]-Neurotensin](http://file.medchemexpress.eu/product_pic/hy-p3057.gif)
![[Phe8Ψ(CH-NH)Arg9]-Bradykinin](http://file.medchemexpress.eu/product_pic/hy-103292.gif)
![[Pyr1]-Apelin-13, Gly(15N) TFA](http://file.medchemexpress.eu/product_pic/hy-p1033s.gif)
![[DPro5] Corticotropin Releasing Factor, human, rat](http://file.medchemexpress.eu/product_pic/hy-p3684.gif)
![Lys-[Des-Arg9]Bradykinin](http://file.medchemexpress.eu/product_pic/hy-103295.gif)
![[Pyr1]-Apelin-13, Pro(13C5,15N) TFA](http://file.medchemexpress.eu/product_pic/hy-p1033s1.gif)
![Lys-[Des-Arg9]Bradykinin TFA](http://file.medchemexpress.eu/product_pic/hy-103295a.gif)
![[Ala1,3,11,15]-Endothelin (53-63)](http://file.medchemexpress.eu/product_pic/hy-p1019.gif)
![Sar-[D-Phe8]-des-Arg9-Bradykinin](http://file.medchemexpress.eu/product_pic/hy-103291.gif)
![[D-Trp8]-γ-MSH](http://file.medchemexpress.eu/product_pic/hy-p1217.gif)
![[Ala1,3,11,15]-Endothelin (53-63) (TFA)](http://file.medchemexpress.eu/product_pic/hy-p1019a.gif)
![D[LEU4,LYS8]-VP](http://file.medchemexpress.eu/product_pic/hy-p1163.gif)
![[D-Trp8]-γ-MSH TFA](http://file.medchemexpress.eu/product_pic/hy-p1217a.gif)
![D[LEU4,LYS8]-VP TFA](http://file.medchemexpress.eu/product_pic/hy-p1163a.gif)
![[Nphe1]Nociceptin(1-13)NH2](http://file.medchemexpress.eu/product_pic/hy-p1320.gif)
![[Nphe1]Nociceptin(1-13)NH2 TFA](http://file.medchemexpress.eu/product_pic/hy-p1320a.gif)
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide](http://file.medchemexpress.eu/product_pic/hy-p1324.gif)
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA](http://file.medchemexpress.eu/product_pic/hy-p1324a.gif)
![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](http://file.medchemexpress.eu/product_pic/hy-p3849.gif)
