Losartan Carboxylic Acid

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Chemical Structure| 124750-92-1 同义名 : E-3174; EXP-3174
CAS号 : 124750-92-1
货号 : A401868
分子式 : C22H21ClN6O2
纯度 : 97%
分子量 : 436.89
MDL号 : MFCD00871928
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Losartan Carboxylic Acid (E-3174), the active metabolite of Losartan featuring carboxylic acid, acts as an antagonist to the angiotensin II receptor type 1 (AT1). It displays Ki values of 0.97, 0.57, and 0.67 nM for rat AT1B/AT1A and human AT1, respectively. This compound inhibits angiotensin II-induced effects in vascular smooth muscle cells (VSMC) and increases plasma renin activity while lowering mean arterial pressure[1][2][3][4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.44mL

2.29mL

1.14mL

22.89mL

4.58mL

2.29mL

参考文献

[1]Sachinidis A, et al. EXP3174, a metabolite of losartan (MK 954, DuP 753) is more potent than losartan in blockingthe angiotensin II-induced responses in vascular smooth muscle cells. J Hypertens. 1993 Feb;11(2):155-62.

[2]Inada Y, et al. Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors. Fundam Clin Pharmacol. 2002 Aug;16(4):317-23.

[3]Richard V, et al. Comparison of the effects of EXP3174, an angiotensin II antagonist and enalaprilat on myocardial infarct size in anaesthetized dogs. Br J Pharmacol. 1993 Nov;110(3):969-74.

[4]Lynch JJ Jr, et al. EXP3174, the AII antagonist human metabolite of losartan, but not losartan nor the angiotensin-converting enzyme inhibitor captopril, prevents the development of lethal ischemic ventricular arrhythmias in a canine model of recent myoca