Losartan Potassium

製品コードS1359 バッチS135904

印刷

化学情報

Chemical Structure Synonyms MK 954,DuP 753 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H23ClKN6O
分子量 462.01 CAS No. 124750-99-8
Solubility (25°C)* 体外 DMSO 92 mg/mL (199.12 mM)
Water 92 mg/mL (199.12 mM)
Ethanol 92 mg/mL (199.12 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
Saline

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 30.000mg/ml (64.93mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ロサルタンカリウムはアンジオテンシンII受容体拮抗薬であり、AT1受容体へのアンジオテンシンIIの結合と競合し、IC50は20 nMです。
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.
特徴 Losartan has a major active metabolite, EXP 3174.

プロトコル(参考用のみ)

動物実験 動物モデル Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ
投薬量 180 mg/d
投与方法 Dietary

参考

  • https://pubmed.ncbi.nlm.nih.gov/11171802/
  • https://pubmed.ncbi.nlm.nih.gov/10747353/
  • https://pubmed.ncbi.nlm.nih.gov/16601194/
  • https://pubmed.ncbi.nlm.nih.gov/10690290/
  • https://pubmed.ncbi.nlm.nih.gov/7475048/

カスタマーフィードバック

, , 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]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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