Ranolazine 2HCl

製品コードS1425 バッチS142505

印刷

化学情報

Chemical Structure Synonyms RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H33N3O4.2HCl
分子量 500.46 CAS No. 95635-56-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.81 mM)
Water 100 mg/mL (199.81 mM)
Ethanol 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.

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生物活性

製品説明 Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
in vitro

Ranolazine selectively inhibits late I(Na), reduces [Na(+)](i)-dependent calcium overload and attenuates the abnormalities of ventricular repolarisation and contractility that are associated with ischaemia/reperfusion and heart failure in myocardial cells. [1] Ranolazine significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. Ranolazine at 5 and 10 mM reversibly shortens the duration of twitch contractions (TC) and abolished the after contraction. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL). [2]
in vivo

Ranolazine (10 mM) significantly increases glucose oxidation 1.5-fold to 3-fold under conditions in which the contribution of glucoseto overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working hearts. Ranolazine similarly increases glucose oxidation in normoxic Langendorff hearts (high Ca, low FA; 15 mL/min). Ranolazine also significantly increases it during flow reduction to 7 mL/min, 3 mL/min, and 0.5 mL/min. Ranolazine significantly improves functional outcome, which is associated with significant increases in glucoseoxidation, a reversal of the increased FA oxidation seen in control reperfusions (versus preischemic), and a smaller but significant increase in glycolysis in reperfuse dischemic working hearts. [3]

プロトコル(参考用のみ)

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：

The antianginal ranolazine fails to improve glycaemia in obese liver-specific pyruvate dehydrogenase deficient male mice [ Basic Clin Pharmacol Toxicol, 2023, 133(2):194-201] PubMed: 37269153
MCL-1 is a master regulator of cancer dependency on fatty acid oxidation [ Cell Rep, 2022, 41(1):111445] PubMed: 36198266
Antiarrhythmic Properties of Ranolazine: Inhibition of Atrial Fibrillation Associated TASK-1 Potassium Channels [ Front Pharmacol, 2019, 10:1367] PubMed: 32038227

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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