Search Result
Results for "
Antagonism
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-13290
-
|
CaMK
P2X Receptor
|
Metabolic Disease
Cancer
|
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
-
- HY-50674
-
INCB3344
Maximum Cited Publications
22 Publications Verification
|
CCR
|
Inflammation/Immunology
Endocrinology
|
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
-
- HY-50674A
-
|
CCR
|
Inflammation/Immunology
|
INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity .
|
-
-
- HY-77111
-
|
Others
|
Inflammation/Immunology
Endocrinology
|
cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
-
- HY-149387
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
-
- HY-149386
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
-
- HY-19012
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
N-1518 is an α and β adrenergic receptor blocker that has competitive antagonism against β1 and α1 receptors, but does not show selectivity for β1 receptors, but shows about 20-fold selectivity for α1 receptors. N-1518 has vasodilatory effects and can be used in the research field of hypertension treatment .
|
-
-
- HY-120301
-
-
-
- HY-P5175
-
|
mAChR
|
Neurological Disease
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
-
- HY-159080
-
|
Parasite
|
Infection
|
HgCht2-IN-1 (compound 1516b) is a HgCht2 inhibitor that successfully inhibits the antagonism of cyst nematodes against nitrogen-fixing rhizobia and phosphate-absorbing arbuscular mycorrhizal symbionts. HgCht2-IN-1 can be used in the study of cyst nematode antagonism against microbial symbionts .
|
-
-
- HY-120188
-
|
PPAR
|
Others
|
CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
|
-
-
- HY-124910
-
-
-
- HY-115844
-
-
-
- HY-136880
-
Sgd 195/78
|
5-HT Receptor
|
Cardiovascular Disease
|
Flufylline shows antihypertensive properties in spontaneously hypertensive rats and display antagonism towards 5-HT receptors in various animal models. Flufylline can be used for cardiovascular disease research .
|
-
-
- HY-164128
-
|
Others
|
Others
|
AHL modulator-1 (compound 12) is a modulator of N-acylated L-homoserine lactone (AHL), with the agonism and antagonism of 21% and 42% in cellulase activity and 5% and 32% in potato macerationa, respectively .
|
-
-
- HY-W650803
-
A-57219
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Nemazoline (A-57219) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
|
-
-
- HY-163703
-
|
Dopamine Receptor
|
Neurological Disease
|
D4R antagonist-2 (compound 33) is a D4R antagonist. D4R antagonist-2 has a IC50 value of 210 nM, and a Ki value of 59 nM for D4R. D4R antagonist-2 can be used in the Parkinson's disease research .
|
-
-
- HY-142066
-
|
PKA
ERK
iGluR
|
Neurological Disease
|
4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling .
|
-
-
- HY-16039
-
|
LPL Receptor
|
Inflammation/Immunology
|
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
|
-
-
- HY-125839
-
|
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
|
-
-
- HY-N7740
-
|
P2Y Receptor
Endogenous Metabolite
|
Others
|
Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors .
|
-
-
- HY-113906A
-
|
GHSR
|
Metabolic Disease
|
(αR,8aS)-GSK1614343 is the isomer of GSK1614343 (HY-113906). GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors .
|
-
-
- HY-P0262A
-
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
-
- HY-161896
-
|
Others
|
Neurological Disease
|
Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models .
|
-
-
- HY-101908
-
|
CCR
|
Inflammation/Immunology
Endocrinology
|
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM) .
|
-
-
- HY-136299A
-
FUT-187
|
iGluR
|
Neurological Disease
|
Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
|
-
-
- HY-161273
-
|
TRP Channel
|
Neurological Disease
|
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .
|
-
-
- HY-117881
-
|
Opioid Receptor
|
Neurological Disease
|
CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
|
-
-
- HY-136299
-
FUT-187 free base
|
iGluR
|
Neurological Disease
|
Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7?μM .
|
-
-
- HY-119971
-
|
Nuclear Hormone Receptor 4A/NR4A
|
Metabolic Disease
Cancer
|
BIM5078 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BIM5078 represses insulin promoter activity through HNF4α antagonism. BIM5078 can be used for the research of cancer and diabetes .
|
-
-
- HY-W424730
-
|
Others
|
Others
|
HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
|
-
-
- HY-108469
-
BI-6015
3 Publications Verification
|
Orphan Receptor
|
Metabolic Disease
Cancer
|
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes .
|
-
-
- HY-P10571
-
|
Melanocortin Receptor
|
Endocrinology
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
-
- HY-155706
-
|
Opioid Receptor
Dopamine Receptor
|
Inflammation/Immunology
|
MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
|
-
-
- HY-13499
-
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
|
-
-
- HY-156734
-
|
SARS-CoV
Virus Protease
|
Infection
|
D-4-77 is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 0.95 μM. D-4-77 has antiviral active with an EC50 value of 0.49 μM. D-4-77 suppresses SARS-CoV-2 Mpro -induced antagonism of the host NF-κB innate immune response .
|
-
-
- HY-P1812
-
AUNP-12
3 Publications Verification
NP-12
|
PD-1/PD-L1
|
Cancer
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
-
- HY-144608
-
|
Opioid Receptor
|
Neurological Disease
|
Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
|
-
-
- HY-148038
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
|
-
-
- HY-101725
-
Ro 11-3128; Ro 11-3128/002
|
Parasite
|
Infection
Neurological Disease
|
Meclonazepam (Ro 11-3128) is a benzodiazepine compound with anxiolytic effect . Meclonazepam is active against immature S. mansoni. Meclonazepam (30 μM) eliminates 100% of immature parasites. Meclonazepam has a anti-schistosomal effect .
|
-
-
- HY-P1812A
-
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
-
- HY-144286
-
|
CXCR
|
Infection
|
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
|
-
-
- HY-121037
-
EGM1
|
Phosphodiesterase (PDE)
|
Cancer
|
Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
|
-
-
- HY-151481
-
|
FXR
|
Metabolic Disease
|
FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
|
-
-
- HY-B1901
-
(±)-Eperisone hydrochloride
|
Others
|
Neurological Disease
|
Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
|
-
-
- HY-144609
-
|
Opioid Receptor
|
Neurological Disease
|
Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
|
-
-
- HY-144607
-
|
Opioid Receptor
|
Neurological Disease
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
|
-
-
- HY-107564
-
VUF 4702 dihydrobromide
|
Histamine Receptor
|
Inflammation/Immunology
|
Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .
|
-
-
- HY-A0081
-
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
-
- HY-119980
-
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980B
-
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-131337
-
|
Bacterial
|
Infection
|
RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections . RhlR antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-119980A
-
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980S
-
|
Isotope-Labeled Compounds
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Others
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980BS
-
|
Isotope-Labeled Compounds
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-A0081R
-
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-101317A
-
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
|
-
- HY-118775
-
|
5-HT Receptor
|
Others
|
LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
|
-
- HY-103164A
-
CSC
|
Others
|
Neurological Disease
|
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitory activity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .
|
-
- HY-19633A
-
|
Others
|
Neurological Disease
|
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0262A
-
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
- HY-P1812
-
AUNP-12
3 Publications Verification
NP-12
|
PD-1/PD-L1
|
Cancer
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-P1812A
-
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-120301
-
-
- HY-P5175
-
|
mAChR
|
Neurological Disease
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- HY-P10571
-
|
Melanocortin Receptor
|
Endocrinology
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-119980S
-
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
-
- HY-119980BS
-
|
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: