| 中文名称: | 司他生坦钠 | ||||
|---|---|---|---|---|---|
| 英文名称: | Sitaxsentan sodium | ||||
| 别名: | 西他塞坦钠;西他生坦钠 IPI 1040 sodium; TBC11251 sodium | ||||
| CAS No: | 210421-74-2 | 分子式: | C18H14ClN2NaO6S2 | 分子量: | 476.89 |
| CAS No: | 210421-74-2 | ||||
| 分子式: | C18H14ClN2NaO6S2 | ||||
| 分子量: | 476.89 | ||||
基本信息
|
产品编号： |
S10589 |
||||
|
产品名称： |
Sitaxsentan sodium |
||||
|
CAS: |
210421-74-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
|
||||
|
分子式： |
溶于液体 |
-80℃ |
6个月 |
||
|
分子量： |
476.89 |
-20℃ |
1个月 |
||
|
化学名： |
|||||
|
Solubility (25°C)： |
|||||
|
体外:
|
DMSO |
|
|||
|
Ethanol |
|
||||
|
Water |
|
||||
|
体内(现配现用): |
|
||||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.0969mL |
10.4846mL |
20.9692mL |
|
5mM |
0.4194mL |
2.0969mL |
4.1938mL |
|
10mM |
0.2097mL |
1.0485mL |
2.0969mL |
生物活性
|
产品描述 |
一种有效的，选择性的 endothelin A receptor 拮抗剂。 |
|
靶点 |
Endothelin Receptor |
|
体外研究 |
Sitaxsentan and Bosentan attenuate NTCP transport at higher concentrations,and inhibit human hepatic transporters,which provides a potential mechanism for the increased hepatotoxicity observed for these agents in the clinical setting.Only sitaxsentan decreased OATP transport (52%).Sitaxsentan and sitaxsentan combined with sildenafil completely prevent the increased expressions of endothelin-1 and of the ETB receptor.Sitaxsentan alone partially restores the expressions of BMPR-1A and BMPR-2.The combination of sildenafil and sitaxsentan further restores the expressions of BMPR-1A and BMPR2,which remaines, however, decreased compared with controls. |
|
体内研究 |
Sitaxsentan (5mg/kg infused iv 10 min prior to onset of hypoxia) completely blocks hypoxia-induced vasoconstriction and this group does not differ from air controls.Oral administration of sitaxsentan,significantly attenuates the increase in MPAP,while the administration of sitaxsentan to rats exposed to normal oxygen levels is without effect on MPAP.Sitaxsentan alone limits shunt-induced increase in MT.Sitaxsentan combined with sildenafil more effectively prevents this remodeling,which,however,tends to remain increased compared with controls. |
推荐实验方法(仅供参考)
|
动物实验: |
|
|
After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30mg/kg body weight per day in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia.At the conclusion of the 4 week period of hypoxia,femoral and pulmonary arterial cannulation and measurement of MPAP, MSAP,and HR are performed. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
