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司他生坦钠  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（100 mg/mL超声）
产品描述：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： C18H14ClN2NaO6S2 溶于液体 -80℃ 6个月 分子量： 476.89 -20℃ 1个月 化学名：  Sodium (4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide 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.
保存条件：-20℃

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