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Sparsentan  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（250mg/mL 超声）
产品描述：基本信息 产品编号： S10848 产品名称： Sparsentan CAS: 254740-64-2   储存条件 粉末 -20℃ 四年     分子式： C32H40N4O5S 溶于液体 -80℃ 6个月 分子量： 592.75 -20℃ 1个月 化学名：  2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide Solubility (25°C)：   体外:   DMSO 100mg/mL (168.7mM) Ethanol 40mg/mL (67.48mM) Water Insoluble 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 1.6871mL 8.4353mL 16.8705mL 5mM 0.3374mL 1.6871mL 3.3741mL 10mM 0.1687mL 0.8435mL 1.6871mL 50mM 0.0337mL 0.1687mL 0.3374mL   生物活性 产品描述 一种高度选择的血管紧张素 II (angiotensin II) 和内皮素 A (endothelin A) 受体的双重拮抗剂，Ki 值分别为 0.8 和 9.3nM。 靶点 Ki:0.8nM (Human angiotensin II),9.3nM (Human endothelin A),0.4nM (Rat angiotensin II) 体内研究 Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 value of 0.8µmol/kg iv and 3.6µmol/kg po.Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model.Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10µmol/kg/day) in spontaneously hypertensive rats.Sparsentan shows good oral bioavailability in rats,dogs,and monkeys, averaging 40%,86%,and 21% F,respectively.At 100µmol/kg/day,Sparsentan reduces the blood pressure from 170 to less than 100mmHg during the course of the drug’s pharmacokinetic duration.Sparsentan at 100µmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration.   推荐实验方法(仅供参考) 动物实验:   Rats:Rats are gavaged with vehicle,and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response.Irbesartan (30µmol/kg) and Sparsentan (30µmol/kg) are given by oral gavage (po),and the rats are re-challenged with angiotensin II at various intervals up to 240 min.There are 6-8 rats per drug dose.The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect.
保存条件：-20℃

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