Product apis-gpcr-g-protein

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Catalog	name	Description	price
R-C-1434	GSK137647A CAS：349085-82-1	GSK137647A is an agonist of the free fatty acid receptor 4(FFA4/GPR120)with pEC50s=6.3,6.2,and 6.1 at human,mouse,and rat receptors,respectively.GSK137647A is selective for GPR120 over a panel of 61 other targets,including other FFARs.	price>
R-R-3134	Gamma-Mangostin CAS No.31271-07-5	Gamma-Mangostin/CAS No.31271-07-5 is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .	price>
R-R-3135	Roluperidone CAS No.359625-79-9	Roluperidone (CYR-101)/CAS No.359625-79-9 is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).	price>
R-R-3136	Syk Inhibitor II CAS No.726695-51-8	Syk Inhibitor II/CAS No.726695-51-8 is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.	price>
R-R-3137	R 59-022 CAS No.93076-89-2	R 59-022 (DKGI-I)/CAS No.93076-89-2 is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.	price>
R-C-1438	CYM5442 CAS：1094042-01-9	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).	price>
R-R-3138	Paliperidone palmitate CAS No.199739-10-1	Paliperidone palmitate (9-Hydroxyrisperidone palmitate)/CAS No.199739-10-1, an atypical long-acting antipsychotic agent, is an ester proagent of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.	price>
R-R-3139	Prucalopride succinate CAS No.179474-85-2	Prucalopride succinate/CAS No.179474-85-2 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.	price>
R-R-3140	Rotigotine CAS No.99755-59-6	Rotigotine/CAS No.99755-59-6 is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor.	price>
R-R-3141	Granisetron Hydrochloride CAS No.107007-99-8	Granisetron (Hydrochloride) (BRL 43694A)/CAS No.107007-99-8 is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.	price>

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