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ZD-1611  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号：Z10063 产品名称：ZD-1611 CAS: 186497-38-1   储存条件 粉末 -20℃ 四年 分子式： C22H24N4O5S 溶于液体 -80℃ 两年 分子量： 456.51     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。   生物活性 产品描述 一种有效的，可口服的，选择性的 ETA receptor 拮抗剂，可用于缺血性脑中风的研究。 靶点/IC50 Endothelin Receptor   体外研究 ZD1611 competitively inhibits 125I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor. 体内研究 ZD1611 (0.3mg/kg,p.o.) has a duration of action of more than 7h in rats. In the dog,ZD1611 is active for at least 6h at dose of 0.6mg/kg p.o.ZD1611 (0.15mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats.However,ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores.   推荐实验方法(仅供参考) 动物实验:   The precursor of ET-1,big ET-1,is used for in vivo analysis of the effects of ZD1611.Exogenously administered big ET-1 is converted to the biologically active peptide ET-1 in vivo via a phosphoramidon-sensitive ET-converting enzyme.In the present study,the use of big ET-1 in vivo is preferred because this compound fails to elicit the initial depressor response associated with i.v.administered ET-1 and yields a greater maximum response than that to ET-1 itself.A partial cumulative dose-response curve to i.v.big ET-1 starting at 0.3nmol/kg) is constructed until pressor responses >30 mm Hg are achieved.After a 55-min recovery period,ZD1611 (0.03-0.3mg/kg) or vehicle is administered,and the big ET-1-response curve is repeated 5 min later.The activity of ZD1611 is calculated as a ratio of the dose of big ET-1 required to give a 30-mm Hg rise in MAP in the absence and then the presence of the compound.
保存条件：-20℃

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