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Tezosentan  

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包装规格：25mg 50mg 100mg in glass bottle
产品描述：基本信息 产品编号： T10856 产品名称： Tezosentan CAS: 180384-57-0   储存条件 粉末 -20℃ 四年 分子式： C27H27N9O6S 溶于液体 -80℃ 二年 分子量 605.63     化学名：  5-Isopropyl-pyridine-2-sulfonic acid {6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-[2-(1H-tetrazol-5-yl)-pyridin-4-yl]-pyrimidin-4-yl}-amide 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。   生物活性 产品描述 一种内皮素 (ET) 受体的一个拮抗剂，其对 ETA 和 ETB 受体的 pA2 值分别为 9.5,7.7。 靶点 ETA 9.5 (pA2) ETB 7.7 (pA2)   体外研究 Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues.Tezosentan inhibits the specific 125Ilabeled ET-1 binding to ETA receptors with an inhibitory potency (Ki) of 0.3nM on CHO cells and of 18nM on membranes of baculovirus-infected insect cells.Similarly,Tezosentan inhibits the specific binding of 125I-labeled ET-1,ET-3,or sarafotoxin S6c to ETB receptors with an inhibitory affinity of 10 to 21nM.Tezosentan up to a concentration of 1μM 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 (1μM) induces a weak inhibition of less than 20%. 体内研究 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 1mg/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.   推荐实验方法(仅供参考) 动物实验:   Rats A pseudocrush syndrome is simulated by injection of i.m.glycerol.A control group does not receive glycerol and is used as a reference.Tezosentan or bosentan for comparison or saline as control is injected as two bolus i.v.doses of 10mg/kg 1h and 20 min before glycerol.Rats are allowed to recover for 2h and then are placed in individual metabolic cages for 48h.Blood samples withdraw from a catheter placed in the abdominal aorta and urine free of food and feces are collected at 24 and 48h.Plasma and urinary creatinine levels are measured with a centrifugal analyzer.Renal function is assessed by calculating creatinine clearance at 24 and 48h after glycerol administration.
保存条件：-20℃

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