CAS NO: | 114798-26-4 |
生物活性 | Losartan is anangiotensin II receptorantagonist, competing with the binding of angiotensin II to AT1 receptors withIC50of 20 nM. | ||||||||||||||||
IC50& Target | 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[1]. Losartan (40 μM) affectsISCbut prevents the effect of ANGII onISC[2]. 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[3]. | ||||||||||||||||
体内研究 (In Vivo) | Losartan (0.6 g/L, p.o.) -treatedFbn1C1039G/+mice show a reduction in distal airspace caliber relative to placebo-treatedFbn1C1039G/+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 ofFbn1C1039G/+mice. Losartan can improve disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics[4]. 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[5]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 422.91 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H23ClN6O | ||||||||||||||||
CAS 号 | 114798-26-4 | ||||||||||||||||
中文名称 | 氯沙坦;洛沙坦;络沙坦 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(236.46 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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