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Ranolazine 2HCl

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Chemical Structure| 95635-56-6 同义名 : 盐酸雷诺嗪;雷诺嗪二盐酸盐 ;CVT 303 dihydrochloride;RS 43285;Ranolazine (hydrochloride);Ranolazine 2HCl
CAS号 : 95635-56-6
货号 : A730331
分子式 : C24H35Cl2N3O4
纯度 : 98%
分子量 : 500.458
MDL号 : -
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(99.91 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(99.91 mM)
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Ranolazine 2HCl is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine ER (Extended-release) was generally well tolerated, with the most commonly reported adverse events including dizziness, nausea, asthenia and constipation[3]. Ranolazine antagonizes the ventricular repolarization changes caused by clofilium and suppresses clofilium-induced TdP (Torsade de Pointes) in rabbits[4]. Ranolazine reduces cellular acetyl-CoA content via inhibition of fatty acid beta-oxidation and activates pyruvate dehydrogenase. Ranolazine (bolus injection: 10 mg/kg plus infusion: 9.6 mg/kg/h, n=12) significantly reduces (i) infarct size and (ii) cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion[5]. Ranolazine improved learning and long-term memory in HFD/STZ + Ranolazine compared to HFD/STZ + Vehicle and ameliorated the pro-inflammatory profile of diabetic mice[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.98mL

4.00mL

2.00mL
参考文献

[1]Undrovinas AI, Belardinelli L, et al. Ranolazine improves abnormal repolarization and contraction in left ventricular myocytes of dogs with heart failure by inhibiting late sodium current. J Cardiovasc Electrophysiol. 2006 May;17 Suppl 1:S169-S177.

[2]Belardinelli L, Shryock JC, et al. Inhibition of the late sodium current as a potential cardioprotective principle: effects of the late sodium current inhibitor ranolazine. Heart. 2006 Jul;92 Suppl 4:iv6-iv14.

[3]Keating GM. Ranolazine: a review of its use as add-on therapy in patients with chronic stable angina pectoris. Drugs. 2013 Jan;73(1):55-73

[4]Wang WQ, Robertson C, Dhalla AK, Belardinelli L. Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits. J Pharmacol Exp Ther. 2008 Jun;325(3):875-81

[5]Zacharowski K, Blackburn B, Thiemermann C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur J Pharmacol. 2001 Apr 20;418(1-2):105-10

[6]Cassano V, Leo A, Tallarico M, Nesci V, Cimellaro A, Fiorentino TV, Citraro R, Hribal ML, De Sarro G, Perticone F, Sesti G, Russo E, Sciacqua A. Metabolic and Cognitive Effects of Ranolazine in Type 2 Diabetes Mellitus: Data from an in vivo Model. Nutrients. 2020 Jan 31;12(2):382