Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC 50 of 20 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 20 nM (angiotensin II)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Losartan (0.6 g/L, p.o.) -treated Fbn1 mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1 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 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. has not independently confirmed the accuracy of these methods. They are for r
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Burnier, M. Angiotensin II type 1 receptor blockers. Circulation, 2001. 103(6): p. 904-12.[2]. Ashry, O., et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol, 2014.[3]. Choi, C.H., et al. Angiotensin II type I receptor and miR-1