Losartan Potassium

製品コードS1359 バッチS135902

印刷

化学情報

 Chemical Structure Synonyms MK 954,DuP 753 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C22H23ClKN6O

分子量 462.01 CAS No. 124750-99-8
Solubility (25°C)* 体外 DMSO 92 mg/mL (199.12 mM)
Water 92 mg/mL (199.12 mM)
Ethanol 92 mg/mL (199.12 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
in vivo Losartan (180 mg/d) causes significant increases in plasma angiotensin II and angiotensin-(1-7) in monkeys with diet-induced hypercholesterolemia. Losartan (180 mg/d) reduces the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% in monkeys with diet-induced hypercholesterolemia. Losartan reduces the susceptibility of LDL to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression in monkeys with diet-induced hypercholesterolemia. [2] Losartan (0.6 g/L in their drinking water) prevents elastic fiber fragmentation and blunted TGF-β signaling in the aortic media in pregnant Fbn1C1039G/+ mice, as evidenced by reduced nuclear accumulation of pSmad2. Losartan (0.6 g/L in their drinking water) shows a reduction in distal airspace caliber in pregnant Fbn1C1039G/+ mice. Losartan (0.6 g/L in their drinking water) improves disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics in pregnant Fbn1C1039G/+ mice. [3] Losartan (5 mg/kg/d) leads to a significant decrease in the development of atherosclerotic lesions in the apo E deficient mice. Losartan (5 mg/kg/d) significantly reduces the susceptibility of the mice LDL to lipid oxidation following its incubation with CuSO4 in the apo E deficient mice. [4] Losartan (10 mg/kg) administration increases blood angiotensin levels four fold to six fold, blood BK levels are unchanged in male Sprague Dawley rats. Losartan (10 mg/kg) increases plasma renin levels 100-fold, plasma angiotensinogen levels decreases to 24% of control and plasma aldosterone levels are unchanged in male Sprague Dawley rats. [5]
特徴 Losartan has a major active metabolite, EXP 3174.

プロトコル(参考用のみ)

動物実験 動物モデル Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ
投薬量 180 mg/d
投与方法 Dietary

カスタマーフィードバック

, , Sci Rep, 2015, 5:8116.

Data from [Data independently produced by , , Neurotherapeutics, 2018, 15(2):500-510]

Data from [Data independently produced by , , Sci Rep, 2018, 8(1):9302]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Effects of Adjunct Antifibrotic Treatment within a Regenerative Rehabilitation Paradigm for Volumetric Muscle Loss [ Int J Mol Sci, 2023, 24(4)3564] PubMed: 36834976
Multitarget, multiagent PLGA nanoparticles for simultaneous tumor eradication and TME remodeling in a melanoma mouse model [ Drug Deliv Transl Res, 2023, 10.1007/s13346-023-01413-9] PubMed: 37612575
The Plasticity of Nanofibrous Matrix Regulates Fibroblast Activation in Fibrosis [ Adv Healthc Mater, 2021, e2001856] PubMed: 33511795
The Expression Patterns and Roles of Lysyl Oxidases in Aortic Dissection [ Front Cardiovasc Med, 2021, 8:692856] PubMed: 34307505
Anti-ATR001 monoclonal antibody ameliorates atherosclerosis through beta-arrestin2 pathway [ Biochem Biophys Res Commun, 2021, 544:1-7] PubMed: 33516876
Hypogonadal hypertension in male Sprague-Dawley rats is renin-angiotensin system-dependent: role of endogenous androgens [ Biol Sex Differ, 2020, 11(1):48] PubMed: 32843085
Matrix Stiffness Controls Cardiac Fibroblast Activation Through Regulating YAP via AT 1 R [ J Cell Physiol, 2020, 2] PubMed: 32239716
Brain Renin–Angiotensin System Blockade Attenuates Methamphetamine-Induced Hyperlocomotion and Neurotoxicity [Jiang L Neurotherapeutics, 2018, 15(2):500-510] PubMed: 29464572
Gallic acid improves cardiac dysfunction and fibrosis in pressure overload-induced heart failure [Jin L Sci Rep, 2018, 8(1):9302] PubMed: 29915390
Irbesartan, an FDA approved drug for hypertension and diabetic nephropathy, is a potent inhibitor for hepatitis B virus entry by disturbing Na+-dependent taurocholate cotransporting polypeptide activity [Wang XJ, et al. Antiviral Res, 2015, 120:140-6] PubMed: 26086883

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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