Losartan potassium Inhibitor CAS No. 124750-99-8

Product Name	Losartan potassium
Synonyms	Cozaar, Anin, MK 954, DuP 753
CAS No.	124750-99-8
Molecular Weight	461
Formula	C₂₂H₂₂ClKN₆O
Chemical Structure

Biological activities

Losartan potassium is a potassium salt of losartan. Losartan is a selective, competitive angiotensin II receptor type 1 (AT1) receptor antagonist. Losartan inhibits the specific binding of [¹²⁵I]-angiotensin II to vascular smooth muscle cells (VSMC) with an IC50 of 10 nM. Losartan prevents the angiotensin II-induced elevation of intracellular cytosolic Ca²⁺ concentration with an IC50 of 50 nM. Losartan abolishes the angiotensin II-induced formation of inositolphosphates in VSMC.^[1] Losartan prevents the CYP2C9-associated tolbutamide methylhydroxylation with a K_{ι of 24.5?µM. Losartan prevents CYP1A2- and CYP3A4-associated activities (ethoxyresorufin O-deethylation and testosterone 6β-hydroxylation) with relatively weak affinities.^[2] Losartan prevents aortic aneurysm in a mouse model of marfan syndrome.^[3] Losartan treatment greatly suppresses the myointimal proliferative response.^[4]}

Protocols

In vivo: Losartan is dissolved in distilled water.^[4]

References

[1] Sachinidis A, et al. EXP3174, a metabolite of losartan (MK 954, DuP 753) is more potent than losartan in blocking the angiotensin II-induced responses in vascular smooth muscle cells. J Hypertens. 1993, 11(2): 155-162. 閵嗏偓閵嗏偓 [2] Taavitsainen P, et al. In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists. Eur J Clin Pharmacol. 2000, 56(2): 135-140. 閵嗏偓閵嗏偓 [3] Habashi JP, et al. Losartan, an AT1 antagonist, prevents aortic aneurysm in a mouse model of Marfan syndrome. Science. 2006, 312(5770): 117-121. 閵嗏偓閵嗏偓 [4] Azuma H, et al. Prevention of intimal thickening after endothelial removal by a nonpeptide angiotensin II receptor antagonist, losartan. Br J Pharmacol. 1992, 106(3): 665-671. 閵嗏偓閵嗏偓

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