司他生坦钠 |
| 时间：2023-07-18 来源：化工号 作者：C18H14ClN2NaO6S2 |
| 中文名 | 司他生坦钠
| | 英文名 | Sitaxsentan sodium
| | 别名 | 西他塞坦钠
司他生坦钠
西他生坦钠
心脑血管类原料药
(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
(4-氯-3-甲基异恶唑-5-基)((2-(2-(6-甲基苯并[D][1,3]二氧杂戊环-5-基)乙酰基)噻吩-3-基)磺酰基)胺钠盐
| | 英文别名 | CS-338
Thelin
TBC-11249
TBC-11251 sodium
sitaxentan sodiuM
SITAXSENTAN SODIUM
Sitaxsentan sodium
4-Chloro-3-methyl-5-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thienylsulfonamido]isoxazole sodium salt
Sodium (4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide
| | CAS | 210421-74-2
| | 化学式 | C18H14ClN2NaO6S2
| | 分子量 | 476.89 | | InChI | InChI=1/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1/rC18H14ClN2NaO6S2/c1-9-5-13-14(27-8-26-13)7-11(9)6-12(23)17-15(3-4-29-17)30(24,25)21(22)18-16(19)10(2)20-28-18/h3-5,7H,6,8H2,1-2H3 | | 溶解度 | H2O: soluble10mg/mL (clear solution) | | 存储条件 | room temp | | 外观 | powder | | 颜色 | white to beige | | 产品用途 | Sitaxentan sodium salt | | 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. | | WGK Germany | 3 | | RTECS | XN0296600 |
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