CR6086 ( CR 6086 | CR-6086 )

产品货号. M16966 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

CR6086
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

CR6086 (CR-6086) 是一种有效的选择性前列腺素 E2 受体 4 (EP4) 拮抗剂，Ki 为 16.6 nM（hEP4 受体）。
产品描述

CR6086 (CR-6086) 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; 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; 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.Rheumatoid Arthritis Phase 2 Clinical.
体外实验

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体内实验

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同义词

CR 6086 | CR-6086
通路

GPCR/G Protein
靶点

Prostaglandin Receptor
受体

Prostaglandin Receptor
研究领域

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适应症

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CAS Number

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分子量

494.49
分子式

C26H26F3N2NaO3
纯度

>98% (HPLC)
溶解度

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SMILES

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化学全称

Sodium (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate