product name Losartan Potassium (DuP 753)
Description: Losartan is a selective, non-peptide angiotensin II receptor antagonist, it competes with angiotensin II for binding to AT1 receptors with IC50 of 20 nM. Losartan inhibits the contractile effects of angiotensin II on rabbit aorta and jugular vein (pA2 = 8.27). It is used as an orally active antihypertensive agent. Losartan (180 mg/d) causes significant increases in plasma angiotensin II and angiotensin-(1-7) in monkeys with diet-induced hypercholesterolemia.
References: Circulation. 2001 Feb 13;103(6):904-12; Circulation. 2000 Apr 4;101(13):1586-93.
462.01
Formula
C22H23ClKN6O
CAS No.
124750-99-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 92 mg/mL (199.1 mM)
Water: 92 mg/mL (199.1 mM)
Ethanol: 92 mg/mL (199.1 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
MK 954
other peoduct :
| In Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. 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. 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. |
| Animal model | Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ |
| Formulation & Dosage | Dissolved in 50% dimethylsulfoxide/50% distilled water; 180 mg/d; Taken via diet |
| References | Circulation. 2001 Feb 13;103(6):904-12; Circulation. 2000 Apr 4;101(13):1586-93. |
