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 Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
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]
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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Matrix Stiffness Controls Cardiac Fibroblast Activation Through Regulating YAP via AT 1 R [ J Cell Physiol, 2020, 2] PubMed: 32239716

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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