Sitaxentan sodium
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产品名称:Sitaxentan sodiumCAS:210421-74-2别名：(4-氯-3-甲基-1,2-恶唑-5-基)-[2-[2-(6-甲基-1,3-苯并二氧戊环-5-基)乙酰基]噻吩-3-基]磺酰亚胺钠盐;司他生坦钠;西他塞坦钠/司他生坦钠;西他塞坦钠;心脑血管类原料药;西他生坦钠英文名：Sitaxentan sodium
- 储存条件 room temp
- 溶解度 H2O: soluble10mg/mL (clear solution)
- 颜色white to beige
- 生物活性Sitaxentan sodium是一种选择性的endothelin A receptor (ETA)(内皮素受体A）拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM，比作用于ETB选择性高7000倍。Phase 3。
- 体外研究Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0.
- 体内研究Sitaxentan sodium has a serum half-life in the rat and the dog of 6 hours - 7 hours and 60−100% oral bioavailability. Orally administered Sitaxentan sodium is rapidly absorbed in both the rat and the dog with a t1/2(abs) of 0.7 hours and 0.3 hours, respectively. Peak plasma concentrations occurred between 2 hours and 3 hours postdosing in the rat and between 45 minutes and 90 minutes in the dog. The pulmonary vasoconstrictor response to acute hypoxia (10% O2 for 90 minutes) is prevented with Sitaxentan sodium (5 mg/kg infused i.v. 10 minutes prior to the onset of hypoxia). Sitaxentan sodium delivered i.v. 50 minutes after the onset of hypoxia reverses the established pulmonary vasoconstriction. Sitaxsentan blocks increased plasma endothelin levels. Sitaxsentan dose dependently (10 mg/kg and 50 mg/kg per day in the drinking water) attenuates right ventricular systolic pressure, right heart hypertrophy, and pulmonary vascular remodeling observed 3 weeks after a single subcutaneous injection of monocrotaline. Systemic administration of the ETA receptor antagonist Sitaxentan sodium significantly attenuates cerebral vasospasm after subarachnoid hemorrhage (SAH). Sitaxentan sodium reduces the development of hypoxic pulmonary vasoconstriction (HPV) in the pig. In addition, bolus injection of Sitaxentan sodium reverses already established HPV.
