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Losartan Carboxylic Acid

Cat. No.:YN320641

  • CAS No. :124750-92-1

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    • 参考文献
    • 产品名称: Losartan Carboxylic Acid
      CAS No.: 124750-92-1
      Chemical Name: 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
      Synonyms:E-3174; EXP-3174
      分子量:436.89
      分子式:C₂₂H₂₁ClN₆O₂
      SMILES:O=C(C1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: Losartan Carboxylic Acid (E-3174) 是 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、0.67 nM。Losartan Carboxylic Acid 阻断血管紧张素II诱导的血管平滑肌细胞 (VSMC) 反应。Losartan Carboxylic Acid 升高血浆肾素活性,降低平均动脉压。
      IC50和靶点:
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    • Inada, Y., Nakane, T., and Chiba, S.Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptorsFundam. Clin. Pharmacol.16(4),317-323(2002)

      Yasar, U., Tybring, G., Hidestrand, M., et al.Role of CYP2C9 polymorphism in losartan oxidationDrug Metab. Dispos.29(7),1051-1056(2001)

      Munger, M.A.Use of angiotensin receptor blockers in cardiovascular protection: Current evidence and future directionsPT36(1),22-40(2011)

      Widdop, R.E., Gardiner, S.M., Kemp, P.A., et al.Comparison of the regional haemodynamic effects of the AT1-receptor antagonists, losartan and EXP 3174, in water-deprived Brattleboro ratsBr. J. Pharmacol.108(3),684-688(1993)

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