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Losartan potassium
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Losartan potassium
CAS No. : 124750-99-8
MCE 站:Losartan potassium
产品活性:Losartan potassium (DuP-753 potassium) 是血管紧张素 II 受体 1 型 (AT1)拮抗剂,与血管紧张素 II 与 AT1 的结合竞争,IC50 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 ISC but prevents the effect of ANGII on ISC. 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 Fbn1C1039G/+ mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1C1039G/+ 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 Fbn1C1039G/+ 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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