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Formula | C22H23ClKN6O |
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Molecular Weight | 462.01 | CAS No. | 124750-99-8 | |
Solubility (25°C)* | In vitro | 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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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Targets |
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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] | ||
Features | Losartan has a major active metabolite, EXP 3174. |
Animal Study:[2] |
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, , 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 |
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