目錄:MedChemExpress LLC>>信號(hào)通路>> Losartan | MedChemExpress
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CAS | 114798-26-4 | 純度 | 99.67% |
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分子量 | 422.91 | 分子式 | C??H??ClN?O |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
貨號(hào) | HY-17512 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥 |
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CAS No. : 114798-26-4
MCE 國(guó)際站:Losartan
產(chǎn)品活性:Losartan 是血管緊張素II受體拮抗劑,與血管緊張素II競(jìng)爭(zhēng)性結(jié)合AT1受體,IC50為20 nM。
研究領(lǐng)域:GPCR/G Protein
作用靶點(diǎn):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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