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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-Evatanepag
Evatanepag

Chemical Structure : Evatanepag

CAS No.: 223488-57-1

Evatanepag (CP-533536 free acid, CP533536)

货号: PC-27072Not For Human Use, Lab Use Only.

Evatanepag (CP-533536, CP-533,536) is a highly selective and potent functional EP2 receptor agonist with high affinity to rat EP2 receptor (IC50=50 nM), is >50-fold more selective over EP4 receptor subtype.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Evatanepag (CP-533536, CP-533,536) is a highly selective and potent functional EP2 receptor agonist with high affinity to rat EP2 receptor (IC50=50 nM), is >50-fold more selective over EP4 receptor subtype.
Evatanepag (CP-533536) also shows high selectivity over other prostanoid receptors, including those for prostaglandin D2, prostaglandin F2a, prostacyclin, and thromboxane.
Evatanepag induces intracellular cAMP levels in HEK-293 cells stably transfected with the EP2 receptor with IC50 of 5 nM.
Evatanepag induces changes in total bone area (TBA), total bone mineral content (BMC), and total bone mineral density (BMD) in the rat local injection model.
Evatanepag has the ability to heal canine long bone segmental and fracture model defects without the objectionable side effects of PGE2.

物理化学性质&存储条件

分子量 468.57
分子式 C25H28N2O5S
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

2-(3-((N-(4-(tert-Butyl)benzyl)pyridine-3-sulfonamido)methyl)phenoxy)acetic acid

参考文献

1. Zhou M, et al. An EP2 receptor-selective prostaglandin E2 agonist induces bone healing. Proc Natl Acad Sci U S A. 2003 May 27;100(11):6736-40.

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