Catalog No.
Product Name
Application
Product Information
Citations
-
Thromboxane A2 synthesis inhibitor
Ozagrel is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. -
5-HT antagonist
Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist. -
mGluR5 PAM
VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax. -
neurokinin-1 receptor antagonist
Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. -
Prostaglandin D2 receptor CRTH2 antagonist
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist. -
CCK-A receptor antagonist
Loxiglumide (CR1505) is a cholecystokinin antagonist -
NT Antagonist
SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions. -
AT1 Receptor Blocker
Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension. -
beta2-adrenergic receptor agonist
Salmeterol is a long-acting beta2-adrenergic receptor agonist -
PGF2α/LTB4 production inhibitor
Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM). -
adrenergic agonist
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. -
D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. -
β2-adrenergic receptor
Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties. -
alpha2-adrenoceptor agonist
Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist - Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
-
Prostaglandin Receptor Agonist
Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation. - Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
-
Leukotriene receptor antagonist
Pranlukast is a selective cysteinyl leukotriene receptor antagonist. - Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
-
CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
CRTH2 antagonist
OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist. -
GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
mGlu4 receptors modulator
VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells. -
mGlu4 receptor modulator
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. -
lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. -
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. -
5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
MCH-1 antagonist
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
