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- Angiotensin Receptor
- Losartan Carboxylic Acid
Losartan Carboxylic Acid
An active metabolite of losartan
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包装价格促销价数量
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5mg￥600.00480.00- +
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10mg￥987.00790.00- +
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50mg￥3487.002790.00- +
- 货号: ajci9266
- CAS: 124750-92-1
- 别名: 氯沙坦羧酸,E-3174,EXP-3174
- 分子式: C22H21ClN6O2
- 分子量: 436.9
- 纯度: ＞98%
- 溶解度: ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
- 储存: Store at -20°C
- 库存: 现货
Background
Ki = 5-20 nM
Losartan Carboxylic Acid, also named E-3174, a physiologically active metabolite of losartan, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. AII is the primary mediator of the reninangiotensin system, which regulates the blood pressure and body-fluid balance and may be associated with the development of cardiovascular diseases via increasing contractility and cell growth in vascular smooth muscle cells (VSMC).
In vitro: E-3174 potently blocked the specific binding of [125I]-AII to VSMC isolated from rat aorta. E-3174 was able to dampen the platelet-derived growth factor-induced increase in cell DNA synthesis and protein, which led to the blockade of the AII-induced increase in cell protein [1].
In vivo: Rats were administrated E-3174 intravenously at a dose of l.0 mg/kg. After 6 hours, E-3174 markedly attenuated the cardiovascular effects of AII in rats. E-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2].
参考文献:
[1].? Li, X. & Widdop, R. Angiotensin Type I Receptor Antagonists CY-11974 and EXP 3174 Cause Selective Renal Vasodilatation in Conscious Spontaneously Hypertensive Rats. Clinical Science, 1996; 91(2): 147-154.
[2].? Sachinidis, A., Ko, Y., Weisser, P., zu BricBkwedde, M., Dsing, R., & Christian, R. et al. EXP3174, a metabolite of losartan (MK954, DuP753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. Journal of Hypertension. 1993; 11(2): 155-162.
