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Losartan

CAS No. : 114798-26-4

MCE 国际站：Losartan

产品活性：Losartan 是血管紧张素II 受体拮抗剂，与血管紧张素II竞争性结合 AT1 受体，IC₅₀ 值为 20 nM。

研究领域：GPCR/G Protein

作用靶点：Angiotensin Receptor

In Vitro: Losartan competes with the binding of angiotensin II to AT1 receptors. The concentration that inhibits 50% of the binding of angiotensin II (IC₅₀) is 20 nM. Losartan (40 μM) affects I_SC but prevents the effect of ANGII on I_SC. Losartan significantly reduces Ang II-mediated cell proliferation in endometrial cancer cells. The combination of losartan and anti-miR-155 has a significantly greater antiproliferative effect compared to each drug alone.

In Vivo: Losartan (0.6 g/L, p.o.) -treated Fbn1^C1039G/+ mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1^C1039G/+ animals. The doses of losartan and propranolol are titrated to achieve comparable hemodynamic effects. Analysis of pSmad2 nuclear staining reveals that losartan antagonizes TGF-β signaling in the aortic wall of Fbn1^C1039G/+ mice. Losartan can improve disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics. Losartan (10 mg/kg, intraarterial injection) increases blood angiotensin levels four- to sixfold. Losartan (10 mg/kg, i.p.) increases plasma renin levels 100-fold; plasma angiotensinogen levels decreases to 24% of control; and plasma aldosterone levels are unchanged.

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