CR6086 | EP4 antagonist | Probechem Biochemicals

Chemical Structure : CR6086

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CR6086 (Vorbipiprant, CR-6086)

货号: PC-20854Not For Human Use, Lab Use Only.

CR6086 (Vorbipiprant) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.

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生物&药学活性

CR6086 (Vorbipiprant) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.
CR6086 reduces key cytokine players of RA (IL-6 and VEGF expression in macrophages, IL-23 release from dendritic cells, IL-17 release from Th17 cells) in models of human immune cells in culture.
CR6086 significantly improves all features of arthritis: severity, histology, inflammation and pain in CIA models of RA in rats and mice.
CR6086 is better than the selective COX-2 inhibitor rofecoxib and at least as effective as the JAK inhibitor tofacitinib.

物理化学性质&存储条件

分子量	472.51
分子式	C26H27F3N2O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoic acid

参考文献

1. Caselli G, et al. Arthritis Res Ther. 2018 Mar 1;20(1):39.

CR6086 (Vorbipiprant, CR-6086)

生物&药学活性

物理化学性质&存储条件

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CR6086 (Vorbipiprant, CR-6086)

生物&药学活性

物理化学性质&存储条件

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