Captopril | 卡托普利

MCE 国际站：Captopril

中文名：卡托普利

CAS：62571-86-2

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：Captopril (SQ 14225)，抗高血压药，是一种含硫醇的竞争性口服活性血管紧张素转换酶 (ACE) 抑制剂 (IC₅₀ =0.025 μM)，广泛用于高血压和充血性心力衰竭的研究。 Captopril 也是一种新德里金属-β-内酰胺酶-1 (NDM-1) 抑制剂，IC₅₀ 为 7.9 μM^[1] [2][3]。 IC50 和目标：ACE^[1]。 

体外：卡托普利 (SQ 14225) 已被证明在高血压患者中具有与利尿剂和 β 受体阻滞剂相似的发病率和死亡率益处。卡托普利已被证明可延缓糖尿病肾病的进展，而依那普利和赖诺普利可预防正常白蛋白尿糖尿病患者肾病的发展^[4]。顺式和反式状态的等摩尔比Captopril 存在于溶液中，并且该酶仅选择抑制剂的反式状态，该抑制剂与其底物结合沟槽具有结构和立体电子互补性^[5]。

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研究领域：Metabolic Enzyme/Protease

作用靶点：Angiotensin-converting Enzyme (ACE)

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参考文献：[1]. Tzakos, A.G., et al., The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme. Bioorg Med Chem Lett, 2006. 16(19): p. 5084-7.

[2]. Song, J.C. and C.M. White, Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet, 2002. 41(3): p. 207-24.

[3]. Afrin S, et al. Eritadenine from Edible Mushrooms Inhibits Activity of Angiotensin Converting Enzyme in Vitro. J Agric Food Chem. 2016;64(11):2263-2268.

[4]. Esmaeili S, et al. Captopril/enalapril inhibit promiscuous esterase activity of carbonic anhydrase at micromolar concentrations: An in vitro study. Chem Biol Interact. 2017;265:24-35.

[5]. Li N, et al. Simplified captopril analogues as NDM-1 inhibitors. Bioorg Med Chem Lett. 2014;24(1):386-389.