TEZOSENTAN
![TEZOSENTAN 结构式](https://img.chemicalbook.com/CAS/GIF/180384-57-0.gif)
TEZOSENTAN 性质
熔点 | 198-200° |
---|---|
沸点 | 761.2±70.0 °C(Predicted) |
密度 | 1.432±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 溶于二甲基亚砜 |
酸度系数(pKa) | 2.93±0.10(Predicted) |
形态 | 固体 |
颜色 | 米白色至灰色 |
TEZOSENTAN 用途与合成方法
ET A 9.5 (pA2) |
ET B 7.7 (pA2) |
Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues. Tezosentan inhibits the specific 125 I-labeled ET-1 binding to ETA receptors with an inhibitory potency (K i ) of 0.3 nM on CHO cells and of 18 nM on membranes of baculovirus-infected insect cells. Similarly, Tezosentan inhibits the specific binding of 125 I-labeled ET-1, ET-3, or sarafotoxin S6c to ET B receptors with an inhibitory affinity of 10 to 21 nM. Tezosentan up to a concentration of 1 μM did not exhibit any binding inhibitory activity in 27 radioligand binding assays different from ET binding. On H1 central, 5-hydroxytryptamine2A, and vasopressin V1 receptors, Tezosentan (1 μM) induces a weak inhibition of less than 20%.
In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats.
TEZOSENTAN 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-04-30 | HY-17351 | 1 mg | 3820 | ||
2024-04-30 | HY-17351 | 5 mg | 9550 |