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NS-304(Selexipag)

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NS-304(Selexipag)
结构式
475086-01-2
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中国地区超过5000个高品质化合物库存
应用领域
Selexipag (NS-304) 是一种口服有效的 前列环素 (PGI2) 受体激动剂。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 475086-01-2
名称:
别名: Selexipag;ACT293987,NS304,NS 304,ACT 293987,ACT-293987
SMILES: CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
分子式: C26H32N4O4S
分子量: 496.62
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: NS-304(Selexipag; ACT-293987) is an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. NS-304 is an orally available and potent agonist for the PGI(2) receptor (IP receptor). The inhibition constant (K(i)) of MRE-269 for the human IP receptor was 20 nM; in contrast, the K(i) values for other prostanoid receptors were >2.6 microM. MRE-269 was therefore a highly selective agonist for the IP receptor. The plasma concentrations of MRE-269 remained near peak levels for more than 8 h after oral administration of NS-304 to rats and dogs, and NS-304 increased femoral skin blood flow in rats in a long-lasting manner without affecting the hemodynamics. These findings indicate that NS-304 acts as a long-acting IP receptor agonist in vivo. The continuous vasodilation evoked by NS-304 was not attenuated by repeated treatment, indicating that NS-304 is unlikely to cause severe desensitization of the IP receptor in rats.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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