| 货号 | 15957-1mg |
| 描述 | Losartan (Item No. 10006594) is an antagonist of the angiotensin II receptor, type 1 (AT1) (Ki = 5-20 nM).1 It has an attenuating effect on vein graft atherosclerosis in rabbits and effectively reduces arterial blood pressure in rats.2,3 In humans, losartan controls hypertension while protecting renal function.4 Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.5 Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.6,7,8 When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.8 However, the metabolite has very low oral bioavailability.8 Losartan, but not its metabolite, inhibits platelet aggregation in vitro.9 |
| 别名 | E-3174;EXP-3174; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ji, H.,Leung, M.,Zhang, Y., et al. Differential structural requirements for specific binding of nonpeptide and peptide antagonists to the AT1 angiotensin receptor. Identification of amino acid residues that determine binding of the antihypertensive drug losartan. J. Biol. Chem. 269(24), 16533-16536 (1994). 2.Ge, J.,Huang, D.,Liang, C., et al. Upregulation of lectinlike oxidized low-density lipoprotein receptor-1 expression contributes to the vein graft atherosclerosis: Modulation by losartan. Atherosclerosis 177(2), 263-268 (2004). 3.Xavier, F.E.,Rossoni, L.V.,Alonso, M.J., et al. Ouabain-induced hypertension alters the participation of enothelial factors in α-adrenergic responses differently in rat resistance and conductance mesenteric arteries. Br. J. Pharmacol. 143(1), 215-225 (2004). 4.Caruso, D.,DAvino, M.,Acampora, C., et al. Effects of losartan and chlorthalidone on blood pressure and renal vascular resistance index in non-diabetic patients with essential hypertension and normal renal functions. J. Cardiovasc. Pharmacol. 44(5), 520-524 (2004). 5.Yasar, U.,Tybring, G.,Hidestrand, M., et al. Role of CYP2C9 polymorphism in losartan oxidation. Drug Metabolism and Disposition 29(7), 1051-1056 (2001). 6.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 receptors. Fundamental Clinical Pharmacology 16, 317-323 (2002). 7.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 rats. British Journal of Pharmacology 108(3), 684-688 (1993). 8.Burnier, M. Angiotensin II type 1 receptor blockers. Circulation 103, 904-912 (2001). 9.Munger, M.A. Use of angiotensin receptor blockers in cardiovascular protection: Current evidence and future directions. PT 36(1), 22-40 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 436.9 |
| 分子式 | C22H21ClN6O2 |
| CAS号 | 124750-92-1 |
| 稳定性 | ≥ 2 years |
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