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Synonyms | MK 954,DuP 753 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H23ClKN6O |
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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. |
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. |
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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. |
動物実験 | 動物モデル | Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ |
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投薬量 | 180 mg/d | |
投与方法 | Dietary |
, , 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]
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。