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Sitaxentan sodium

Sitaxentan sodium 更多供应商
公司名称:上海得恩德医药科技有限公司  
联系电话:+86 (21) 58783620
产品介绍:中文名称:(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
英文名称: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
公司名称:百灵威科技有限公司  
联系电话:400-666-7788 +86-10-82848833
产品介绍:英文名称:Sitaxsentan SodiuM
CAS:210421-74-2
包装信息:10Mg,25Mg,50Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称:上海佰世凯化学科技有限公司  
联系电话:+86(0)21-20908456
产品介绍:英文名称:Sitaxsentan sodiuM
CAS:210421-74-2
备注:C14177
公司名称:凯试(上海)科技有限公司  
联系电话:021-50135380
产品介绍:英文名称:Sitaxsentan SodiuM;N-(4-Chloro-3-Methyl-5-isoxazolyl)-2-[2-(6-Methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonaMide
CAS:210421-74-2
纯度:98+% 包装信息:1Mg;5Mg;10Mg;50Mg;100Mg;500Mg 备注:T试剂
公司名称:杭州宇昊化工科技有限公司  
联系电话:0571-82693216
产品介绍:英文名称:sitaxentan sodiuM
CAS:210421-74-2
Sitaxentan sodium
生物活性 体外研究 体内研究
中文名称:Sitaxentan sodium
中文同义词:(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
英文名称:Sitaxentan sodium
英文同义词:SITAXSENTAN SODIUM;Sodium (4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide;TBC-11249;Thelin;sitaxentan sodiuM;N-(4-Chloro-3-Methylisoxazol-5-yl)-2-[2-(6-Methyl-1,3-Benzodioxol-5-yl)acetyl]thiophene-3-sulfonaMide;N-(4-Chloro-3-Methyl-5-isoxazolyl)-2-[2-(6-Methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonaMide;TBC11251 sodiuM salt
CAS号:210421-74-2
分子式:C18H14ClN2NaO6S2
分子量:476.89
EINECS号:
相关类别:Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;原料药标样;Sitaxsentan Sodium;司他生坦钠;心脑血管类科研原料药;医药中间体;G蛋白偶联受体&G蛋白;Inhibitors;小分子抑制剂,天然产物
Mol文件:210421-74-2.mol
Sitaxentan sodium
Sitaxentan sodium 性质
储存条件 room temp
溶解度 H2O: soluble10mg/mL (clear solution)
颜色white to beige
Sitaxentan sodium 用途与合成方法
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.
安全信息
RTECS号XN0296600
"Sitaxentan sodium" 相关产品信息
Sitaxentan sodium