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产品价格:电议      采购度:1591      原产地:美洲
发布时间:2021/7/29 19:22:07 所属地区:上海 上海市
简要描述:
Selexipag (NS-304) 是一种口服有效的 前列环素 (PGI2) 受体激动剂。
标签:NS-304
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CAS No. : 475086-01-2
MCE 站:Selexipag
产品活性:Selexipag (NS-304) 是一种口服有效的 前列环素 (PGI2) 受体激动剂。
研究领域:GPCR/G Protein
In Vitro: Selexipag (NS-304) is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly selective for the IP receptor. Selexipag (NS-304) inhibits the binding of [3H]Iloprost to the human and rat IP receptors in a concentration-dependent manner. The Ki is 260 nM for the human IP receptor and 2100 nM for the rat IP receptor. The intracellular cAMP levels in hIP-CHO cells are increased in a concentration-dependent manner by treatment with Selexipag (NS-304) with EC50 of 177nM. Selexipag (NS-304) also inhibits platelet aggregation in humans and monkeys with IC50 values of 5.5 and 3.4 μM, respectively, but it shows no inhibition in dogs (IC50 of >100 μM).
In Vivo: The Cmax of MRE-269 after oral administration of NS-304 is 1.1 μg/mL in rats and 9.0 μg/mL in dogs. Selexipag (NS-304) at 1 or 3 mg/kg increases FSBF in anesthetized rats for more than 4 h after intraduodenal administration in a dose-dependent manner. In particular, Selexipag (NS-304) at 3 mg/kg causes a sustained increase in FSBF and exhibits a maximal increase of 93% in FSBF 1 h after administration.
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更新时间:2024/1/2 10:17:03
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