公司名称: |
北京百灵威科技有限公司 |
联系电话: |
400-666-7788 010-82848833 |
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: |
021-20908456 |
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
|
公司名称: |
BOC Sciences |
联系电话: |
16314854226 |
产品介绍: |
英文名称:Sitaxentan sodium CAS:210421-74-2
|
|
储存条件 | room temp | 溶解度 | H2O: soluble10mg/mL (clear solution) | 形态 | powder | 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. |
WGK Germany | 3 | RTECS号 | XN0296600 |
|