-
dopamine D2 receptor antagonist
Haloperidol D4 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist. -
5-HT2 receptor antagonist
Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. -
mGluR5 agonist
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. -
dopamine D2 receptor antagonist
Haloperidol-d4-1 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
-
5-HT2 receptor antagonist
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. -
histamine H2-receptor antagonist
Niperotidine is a histamine H2-receptor antagonist. -
dopamine D4 receptor partial agonist
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM. -
serotonin reuptake inhibitor/5-HT2A receptor antagonist
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. -
5-HT / dopamine receptor antagonist
Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
adenosine A1 receptor antagonist
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. -
dopamine D2/D3 receptor antagonist
Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively. -
dual ETA/ETB antagonist
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. -
human 5-HT1A receptor partial agonist
Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. -
histamine H3 receptor antagonist
GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. -
D2R antagonist
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. -
Gastrin/CCK-B antagonist
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. -
CXCR4 antagonist
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. -
δ-opioid receptor modulator
BMS-986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor. -
δ-opioid receptor modulator
BMS-986187 is a potent and selective positive allosteric modulator (PAM) of the δ-opioid receptor and a G-protein-biased allosteric agonist. -
bovine tubulin oxidation inhibitor
Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor. -
histamine H1 receptor antagonist
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. -
antiplatelet activities
6-Methoxydihydroavicine is an alkaloid isolated from Zanthoxylum integrifoliolum. 6-Methoxydihydroavicine has antiplatelet activities and inhibits AA-, collagen- and PAF-induced platelet aggregation in vitro. -
A1 adenosine receptor agonist
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. - SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties.
-
β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
-
histamine H3R antagonist/inverse agonist
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. -
5-HT3 receptor antagonist
5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system. -
CXCR4 antagonist
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM.
GPCR/G Protein
Catalog No.
Product Name
Application
Product Information
Citations
