Selexipag
产品说明书
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同义名 : | 塞乐西帕 ;NS-304; ACT-293987; Uptravi. |
| CAS号 : | 475086-01-2 | |
| 货号 : | A203007 | |
| 分子式 : | C26H32N4O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 496.62 | |
| MDL号 : | MFCD10567093 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Selexipag (NS-304) is an orally administered, long-acting prodrug that acts as an IP receptor agonist. Its active metabolite, MRE-269, exhibits high selectivity for the IP receptor. Selexipag (NS-304) concentration-dependently inhibits the binding of [3H]Iloprost to both human and rat IP receptors, with Ki values of 260 nM and 2100 nM, respectively. Treatment with Selexipag (NS-304) increases intracellular cAMP levels in hIP-CHO cells in a concentration-dependent manner, with an EC50 of 177nM. Additionally, Selexipag (NS-304) inhibits platelet aggregation in humans and monkeys, with IC50 values of 5.5 μM and 3.4 μM, respectively, while exhibiting no inhibition in dogs (IC50 >100 μM) [1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.01mL 0.40mL 0.20mL |
10.07mL 2.01mL 1.01mL |
20.14mL 4.03mL 2.01mL |
| 参考文献 |
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