Home GPCR & G Protein Angiotensin Receptor antagonist Losartan Potassium For research use only.

Losartan Potassium

Synonyms: MK 954,DuP 753

Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

Losartan Potassium Chemical Structure

Losartan Potassium Chemical Structure

CAS No. 124750-99-8

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Losartan Potassium Related Products

Biological Activity

Description Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Features Losartan has a major active metabolite, EXP 3174.
Targets
AT1 receptor [1]
20 nM
In Vivo
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]
Animal Research Animal Models Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ
Dosages 180 mg/d
Administration Dietary
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00880386 Withdrawn
Dyspnea|Lung Cancer|Pulmonary Complications|Radiation Fibrosis
University of South Florida|National Cancer Institute (NCI)
 March 2009 Not Applicable

Chemical Information & Solubility

Molecular Weight 462.01 Formula

C22H23ClKN6O
CAS No. 124750-99-8 SDF Download Losartan Potassium SDF
Smiles CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4)CO)Cl.[K+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 92 mg/mL

Ethanol : 92 mg/mL


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In vivo
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