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Catalog No.
Product Name
Application
Product Information
Product Citation
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nonimidazole inverse agonist
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). -
PAR4 antagonist
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. -
PAF antagonist
Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo. -
5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. -
5-HT4 receptor antagonist
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. -
GPR4 antagonist
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
β3-adrenergic receptor agonist
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). -
NK1 receptor antagonist
GR 205171 is a selective neurokinin-1 receptor antagonist - Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.
- Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
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endothelin receptor modulator
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. -
NK1 receptor antagonist
Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. -
tachykinin NK2 receptor antagonist
Ibodutant is a tachykinin NK2 receptor antagonist for the treatment of Irritable Bowel Syndrome with diarrhoea (IBS-D) -
Oxytocin Receptor Antagonist
Retosiban (GSK-221,149-A) is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptor antagonist with >1400-fold selectivity[3] over the related vasopressin receptors -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. -
guanylate cyclase (sGC) stimulator
Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay. -
CCK-2 receptor antagonist
Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
OX Receptor Antagonist
SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. -
GLP-1 receptor agonist
Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. -
Non-selective β antagonist
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). -
dopamine D2 receptor agonist
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor. -
Sigma-1 receptor antagonist
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (??1) receptor antagonist with a Ki of 1.14 nM. -
sigma 1 receptor antagonist
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, respectively.
