Fimasartan

製品コードS4975 バッチS497501

印刷

化学情報

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

C27H31N7OS
分子量 501.65 CAS No. 247257-48-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.34 mM)
Ethanol 24 mg/mL (47.84 mM)
Water Insoluble
* <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 Fimasartan (Kanarb) is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.
in vitro Fimasartan is a selective AT1 receptor antagonist. The concentration that inhibits the binding of [125I]Ang II to the AT1 receptor from rat adrenal cortex by 50% (IC50) is 0.13 nM. Fimasartan shows superior inhibitory activity in the contraction of isolated rabbit thoracic aorta compared to other ARBs such as losartan and candesartan[1]. Fimasartan potently attenuates myocardial apoptotic death in reperfused rat heart and H9c2 cells. Fimasartan could attenuate mitochondrial damage which is associated with minimizing the reduction in Bcl-2 and connected with the reduction in p53 and activation of Akt and GSK-3β, and inhibiting mitochondrial Ca2+ overload by suppressing the ICa,L and MCU[2].
in vivo In various animal models including renal hypertensive rats, spontaneously hypertensive rats and Beagle dogs, fimasartan effectively reduces blood pressure in a dose-dependent manner following single or repeated oral and intravenous administration. Fimasartan does not affect general behavior, respiratory rate or tidal volume in experimental animals, and shows no adverse findings in the human ether-a-go-go-related gene (hERG) test or monkey telemetry study. A number of general toxicity, carcinogenic toxicity, genetic toxicity, and developmental toxicity studies given either orally or intravenously in various species including mice, rats, monkeys and dogs are conducted and these preclinical results demonstrate the safety and tolerability of fimasartan for long-term clinical use and offer sufficient safety margins to support the expected human therapeutic dose. Fimasartan is rapidly absorbed following oral administration with the time to peak plasma concentration (Tmax) ranging 0.5-3 h and the terminal half-life (t1/2) being 5-16 h at doses of 20 to 480 mg in healthy subjects. Similar results are obtained in patients with hypertension, i.e., Tmax ranges 0.5-1.3 h and t1/2 is 7-10 h following fimasartan administration at doses 20-180 mg in the subsequent phase II study. The urinary excretion of fimasartan is low, with the overall urinary excretion of unchanged drug over the first 24 h after dosing being less than 3% of the administered dose. Fimasartan undergoes nonrenal elimination with minimal metabolism[1]. Fimasartan treatment before myocardial ischemia significantly attenuates reperfusion injury and apoptotic changes, possibly by suppressing mitochondrial damage during reperfusion[2]. In various preclinical studies, including aortic balloon injury, myocardial infarct ischemia/reperfusion, doxorubicin cardiotoxicity, and ischemic stroke models, fimasartan shows anti-inflammatory and organ-protecting effects[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 H9c2 cells
濃度 50 μM
反応時間 24 h
実験の流れ H9c2 cells are pretreated with fimasartan (50 μM) for 24 h prior to experiencing 18-h/48-h reoxygenation.
動物実験 動物モデル Sprague-Dawley rats (animal model with myocardial ischemia/reperfusion injury)
投薬量 3 mg/kg
投与方法 i.v

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Calibrating the In Vitro-In Vivo Correlation for OATP-Mediated Drug-Drug Interactions with Rosuvastatin Using Static and PBPK Models [ Drug Metab Dispos, 2020, 48(12):1264-1270] PubMed: 33037044

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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