別品名 |
DuPont-753, Losaprex, Lortaan, Neo-Lotan, Oscaar, 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'- biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol monopotassium salt
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別包装 |
あり
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純度 |
>=98%
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分子量 |
461.01
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CAS RN® |
124750-99-8
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化合物の概要 |
AT1 antagonist.
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構造 |
C22H22ClN6O K
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溶媒 |
Soluble in water to 100 mM, DMSO to 100 mM, and alcohol.
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使用目的 |
Losartan is an inhibitor of the angiotensin II type 1 (AT1) receptor that exhibits antihypertensive, anti-fibrotic, and nephroprotective activities. In animal models of obstructive nephropathy, losartan decreases levels of α-SMA and collagen type 1 and inhibits phosphorylation of STAT3, suppressing renal tubular fibrosis. Losartan also inhibits the endothelial-to-mesenchymal transition through indirect inhibition of ERK activation, potentially showing anti-fibrotic benefit after myocardial infarction.
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その他 |
[融点]263-265 ℃ [沸点]682℃
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参考文献 |
He P, Li D, Zhang B. Losartan attenuates renal interstitial fibrosis and tubular cell apoptosis in a rat model of obstructive nephropathy. Mol Med Rep. 2014 Aug;10(2):638-44. PMID: 24912579.Wylie-Sears J, Levine RA, Bischoff J. Losartan inhibits endothelial-to-mesenchymal transformation in mitral valve endothelial cells by blocking transforming growth factor-β-induced phosphorylation of ERK. Biochem Biophys Res Commun. 2014 Apr 18;446(4):870-5. PMID: 24632204.Gibson TJ. Hypertension, its treatment, hyperuricaemia and gout. Curr Opin Rheumatol. 2013 Mar;25(2):217-22. PMID: 23370375.Apostolakis S, Krambovitis E, Vlata Z, et al. CX3CR1 receptor is up-regulated in monocytes of coronary artery diseased patients: impact of pre-inflammatory stimuli and renin-angiotensin system modulators. Thromb Res. 2007;121(3):387-395. PMID: 17521710.Koseki N, Deguchi J, Yamashita A, et al. Establishment fo a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish. J Toxicol Sci. 2014 Aug;39(4):579-600. PMID: 25056783.Nagata T, Fukuzawa T, Takeda M, et al. Tofogliflozin, a novel sodium-glucose co-transporter 2 inhibitor, improves renal and pancreatic function in db/db mice. Br J Pharmacol. 2013 Oct;170(3):519-531. PMID: 23751087.
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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