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Losartan potassium

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Chemical Structure| 124750-99-8 同义名 : DuP-753 potassium;Losartan (potassium salt);MK 954;DuP 753
CAS号 : 124750-99-8
货号 : A561984
分子式 : C22H22ClKN6O
纯度 : 98%
分子量 : 461.001
MDL号 : MFCD02092704
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(227.77 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(108.46 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 The numerous effects of Angiotensin II (AII), including its roles in vasoconstriction, secretion of aldosterone and vasopressin, cellular proliferation, and hypertrophy are dominantly mediated through the activation of the angiotensin type 1 (AT1) receptor, a member of the superfamily of G protein-coupled receptors [5]. Losartan Potassium is an AII receptor antagonist that competitively binds the AT1 receptor with IC50 of 20 nM [6]. Male cynomolgus monkeys were given losartan (180 mg/d, n=6) or vehicle (n=8) for 6 weeks. Losartan caused significant (P<0.05) increases in plasma AII and angiotensin-(1-7). Compared with vehicle-treated controls, losartan reduced the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% (P<0.05). A significant (P<0.05) reduction in the susceptibility of low-density lipoprotein (LDL) to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression were also associated with losartan treatment [7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00763893 Marfan Syndrome Phase 3 Terminated(A similar publicati... 展开 >>on has been released, suggesting a beneficial effect of sartans, and only 15 patients remained to be seen for their visit at 36 months.) 收起 << - France ... 展开 >> Hôpital Bichat Paris, France, 75018 收起 <<
NCT01224860 Renal Transplant Phase 2 Completed - Italy ... 展开 >> Mario negri Institute - Clinical Research Center for Rare Diseases Ranica, Bergamo, Italy, 24020 收起 <<
NCT01620788 Hypertension Phase 3 Not yet recruiting March 2019 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.08mL

21.69mL

4.34mL

2.17mL
参考文献

[1]Habashi JP, Judge DP, et al. Losartan, an AT1 antagonist, prevents aortic aneurysm in a mouse model of Marfan syndrome. Science. 2006 Apr 7;312(5770):117-21.

[2]Strawn WB, Chappell MC, et al. Inhibition of early atherogenesis by losartan in monkeys with diet-induced hypercholesterolemia. Circulation. 2000 Apr 4;101(13):1586-93.

[3]Vijayapandi P, Nagappa AN, et al. Biphasic effects of losartan potassium on immobility in mice. Yakugaku Zasshi. 2005 Aug;125(8):653-7.

[4]Zhao Q, Wei J, et al. Effects of quercetin on the pharmacokinetics of losartan and its metabolite EXP3174 in rats. Xenobiotica. 2019 May;49(5):563-568.

[5]Ojima M, Igata H, Tanaka M, Sakamoto H, Kuroita T, Kohara Y, Kubo K, Fuse H, Imura Y, Kusumoto K, Nagaya H. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8. doi: 10.1124/jpet.110.176636. Epub 2010 Dec 1. PMID: 21123673.

[6]Burnier M. Angiotensin II type 1 receptor blockers. Circulation. 2001 Feb 13;103(6):904-12. doi: 10.1161/01.cir.103.6.904. PMID: 11171802.

[7]Strawn WB, Chappell MC, Dean RH, Kivlighn S, Ferrario CM. Inhibition of early atherogenesis by losartan in monkeys with diet-induced hypercholesterolemia. Circulation. 2000 Apr 4;101(13):1586-93. doi: 10.1161/01.cir.101.13.1586. PMID: 10747353.