拉帕司他

• 常用名: 拉帕司他
• 英文名: Lapaquistat Acetate
• CAS号: 189060-13-7
• 分子量: 645.14000
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₃H₄₁ClN₂O₉
• 熔点: N/A
• 闪点: N/A

拉帕司他用途

Lapaquistat acetate (TAK-475) 是一种角鲨烯合酶 (squalene synthase) 抑制剂,可阻止法呢基二磷酸酯 (FPP) 转化为角鲨烯。Lapaquistat acetate (TAK-475) 最初旨在用于甲羟戊酸激酶缺乏症 (MKD),可有效降低低密度脂蛋白胆固醇,但可能引起肝脏损害。

拉帕司他名称

• 中文名: 拉帕司他
• 英文名: 2-[1-[2-[(3R,5S)-1-(3-acetyloxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-5H-4,1-benzoxazepin-3-yl]acetyl]piperidin-4-yl]acetic acid

拉帕司他生物活性

• 描述: Lapaquistat acetate (TAK-475) 是一种角鲨烯合酶 (squalene synthase) 抑制剂,可阻止法呢基二磷酸酯 (FPP) 转化为角鲨烯。Lapaquistat acetate (TAK-475) 最初旨在用于甲羟戊酸激酶缺乏症 (MKD),可有效降低低密度脂蛋白胆固醇,但可能引起肝脏损害。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> 代谢酶/蛋白酶 >> 法呢基转移酶
• 靶点实验:

  Squalene synthase[1]

• 参考文献:

  [1]. Stein EA, et al. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85.

  [2]. Marcuzzi A, et al. Repositioning of Tak-475 In Mevalonate Kinase Disease: Translating Theory Into Practice. Curr Med Chem. 2018;25(24):2783-2796.

拉帕司他物理化学性质

• 分子式: C₃₃H₄₁ClN₂O₉
• 分子量: 645.14000
• 精确质量: 644.25000
• PSA: 131.91000
• LogP: 4.87400
• InChIKey: CMLUGNQVANVZHY-POURPWNDSA-N
• SMILES: COc1cccc(C2OC(CC(=O)N3CCC(CC(=O)O)CC3)C(=O)N(CC(C)(C)COC(C)=O)c3ccc(Cl)cc32)c1OC
• 外观性状: 固体
• 储存条件: 2-8°C，密封，干燥

拉帕司他靶点实验

查看更多实验

实验名称：Concentration required for 50% inhibitory activity against cholesterol synthesis in r... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL819179

实验名称：Lipid lowering effect in marmosets assessed as reduction in plasma HDL-cholesterol le... 来源：ChEMBL 靶标：marmosets External Id：CHEMBL2061367

实验名称：Lipid lowering effect in marmosets assessed as reduction in plasma non HDL-cholestero... 来源：ChEMBL 靶标：marmosets External Id：CHEMBL2061368

实验名称：Lipid lowering effect in marmosets assessed as reduction in plasma total cholesterol ... 来源：ChEMBL 靶标：marmosets External Id：CHEMBL2061366

实验名称：Inhibition of recombinant squalene synthase assessed as conversion of trans,trans-[1-... 来源：ChEMBL 靶标：Squalene synthase External Id：CHEMBL1781817

实验名称：In vivo inhibition of squalene synthase in NMRI rat assessed as inhibition of hepatic... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL1780631

实验名称：Stability in human liver microsomes assessed as compound remaining after 60 mins 来源：ChEMBL 靶标：Liver microsomes External Id：CHEMBL1781818

实验名称：In vivo inhibition of squalene synthase in NMRI rat assessed as inhibition of hepatic... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL1780632

实验名称：Compound at a dose of 1 mg/kg was administered orally to 6 week old male Wistar rats ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL820016

实验名称：Reduction in total cholesterol level in marmosets at 30 mg/kg/day, po for 7 days 来源：ChEMBL 靶标：marmosets External Id：CHEMBL2446436

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拉帕司他英文别名

• Lapaquistat acetate
• UNII-IUH3AY74O3
• TAK-475