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

Chemical Structure : Ralinepag

CAS No.: 1187856-49-0

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Ralinepag (APD811, APD-811)

货号: PC-24814Not For Human Use, Lab Use Only.

Ralinepag (APD811) is a potent, selective, orally bioavailable and non-prostanoid prostacyclin receptor (IP) agonist with EC50 of 8.5 nM and 530 nM for human and rat IP receptors respectively, inhibits ADP-induced human platelet aggregation with IC50 of 38 nM.

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

生物&药学活性

Ralinepag (APD811) is a potent, selective, orally bioavailable and non-prostanoid prostacyclin receptor (IP) agonist with EC50 of 8.5 nM and 530 nM for human and rat IP receptors respectively, inhibits ADP-induced human platelet aggregation with IC50 of 38 nM.
Ralinepag (APD811) has IC50 of 3 nM in radioligand binding assays of affinity for the IP receptor in multiple species, 30- to 50-fold over human EP3, good selectivity in both binding and functional assays with respect to most members of the prostanoid receptor family.
Ralinepag (APD811) significantly reduce the MCT-induced increase in pulmonary arterial pressure in monocrotaline (MCT) model.

物理化学性质&存储条件

分子量 431.91
分子式 C23H26ClNO5
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-((trans-4-((((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetic acid

参考文献

1. Tran TA, et al. J Med Chem. 2017 Feb 9;60(3):913-927.

2. Torres F, et al. Eur Respir J. 2019 Oct 10;54(4):1901030.

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