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

Chemical Structure : Selexipag

CAS No.: 475086-01-2

Selexipag (NS-304, ACT-293987, NS304, ACT293987)

货号: PC-20915Not For Human Use, Lab Use Only.

Selexipag (NS-304) is an orally available, long-acting nonprostanoid prostacyclin receptor (IP receptor) agonist, the prodrug of the active form of MRE-269.

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

生物&药学活性

Selexipag (NS-304) is an orally available, long-acting nonprostanoid prostacyclin receptor (IP receptor) agonist, the prodrug of the active form of MRE-269.
MRE-269 inhibits the human IP receptor with inhibition constant (Ki) of 20 nM.
Selexipag (NS-304) inhibits the binding of [3H]Iloprost to the human and rat IP receptors in a concentration-dependent manner., with Ki of 260 nM for the human IP receptor and 2100 nM for the rat IP receptor.
Selexipag (NS-304) increases intracellular cAMP levels in hIP-CHO cells with EC50 of 177 nM.
Selexipag (NS-304) is a promising drug candidate for various vascular diseases, especially pulmonary arterial hypertension and arteriosclerosis obliterans.

物理化学性质&存储条件

分子量 496.63
分子式 C26H32N4O4S
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-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide

参考文献

1. Morrison K, et al. J Pharmacol Exp Ther. 2010 Oct;335(1):249-55.

2. Kuwano K, et al. J Pharmacol Exp Ther. 2008 Sep;326(3):691-9.

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