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Losartan Carboxylic Acid  ≥98%

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包装规格：10mg 50mg 250mg 1g in glass bottle
溶解性：溶于DMSO(≥250 mg/mL)
产品描述：基本信息 产品编号： L10420  产品名称： Losartan Carboxylic Acid CAS: 124750-92-1   储存条件 粉末 -20℃ 四年     分子式： C22H21ClN6O2 溶于液体 -80℃ 6个月 分子量： 436.89 -20℃ 1个月 化学名：  2-Butyl-4-chloro-1-[(2'-(1-H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl)methyl]-1-H-imidazole-5-carboxylic acid Solubility (25°C)：   体外:   DMSO 87mg/mL (199.13mM) Ethanol 87mg/mL (199.13mM) 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 2.2889mL 11.4445mL 22.8891mL 5mM 0.4578mL 2.2889mL 4.5778mL 10mM 0.2289mL 1.1445mL 2.2889mL 50mM 0.0458mL 0.2289mL 0.4578mL   生物活性 产品描述 一种Losartan 的活性羧酸代谢产物，是血管紧张素 Ⅱ 受体 1 型 (AT1) 拮抗剂。对大鼠 AT1B/AT1A 和人 AT1 的 Ki 值分别为 0.97、0.57、0.67nM。 靶点 binding of [125I]-angiotensin II to VSMC(Cell-free assay) 1.1nM   体外研究 The specific binding of [125I]-angiotensin II to VSMC is inhibited by Losartan Carboxylic Acid (E-3174) with an IC50 of 1.1nM.Losartan Carboxylic Acid abolishes the angiotensin II-induced formation of inositolphosphates in VSMC.Losartan Carboxylic Acid inhibits the angiotensin II-induced elevation of intracellular cytosolic Ca2+concentration with an IC50 of 5nM.Losartan Carboxylic Acid is more effective than losartan in blocking the angiotensin II-induced increase in Egr-1 mRNA.Losartan Carboxylic Acid inhibits the angiotensin II-induced cell protein synthesis with an IC50 of 3nM. 体内研究 Losartan Carboxylic Acid (E-3174) (0.1mg/kg;i.v. followed by 0.02mg/kg/h for 5.5h) induces a similar level of inhibition (87±4%) of the pressor responses to angiotensin I.Intravenous Losartan Carboxylic Acid (0.1mg/kg+0.01mg/kg/min) is infused in anesthetized dogs with recent (8.1±0.4 days) anterior myocardial infarction.Electrolytic injury of the left circumflex coronary artery to induce thrombotic occlusion and posterolateral ischemia is initiated 1h after the start of treatment. Animal Model: Mongrel dogs of either sex, weighing 15-25kg Dosage: 0.1mg/kg (followed by 0.02mg/kg/h) Administration: i.v.for 5.5 hours Result: The pressor response was reduced by 87±4%.
保存条件：-20℃

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