产品说明书

Ranolazine

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Chemical Structure| 95635-55-5 同义名 : CVT 303;RS 43285-003
CAS号 : 95635-55-5
货号 : A103291
分子式 : C24H33N3O4
纯度 : 98%
分子量 : 427.536
MDL号 : MFCD00864690
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(245.59 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Ranolazine 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)[3]. Ranolazine antagonizes the ventricular repolarization changes caused by clofilium and suppresses clofilium-induced TdP (Torsade de Pointes) in rabbits[4]. Ranolazine potentiates the effects of ACEIs (angiotensin-converting enzyme inhibitor) and ARBs (angiotensin receptor blocker). Clinicians should monitor for this potentiation when initiating treatment with ranolazine and an ACEI or ARB[5]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Ranolazine reduces cellular acetyl-CoA content via inhibition of fatty acid beta-oxidation and activates pyruvate dehydrogenase. Ranolazine significantly reduces infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion[6]. Ranolazine therapy may decrease A1C (andhemoglobin A1C) among patients with T2DM without an increase in hypoglycemia. For patients with T2DM (type 2 diabetes mellitus) and chronic stable angina, ranolazine may be of use given its utility in cardiovascular disease and benefit in A1C lowering[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02425969 Grey-zone Fractional Flow Rese... 展开 >>rve Intermediate Coronary Lesions Stable Angina Coronary Physiology 收起 << Not Applicable Completed - United Kingdom ... 展开 >> Golden Jubilee National Hospital Glasgow, Dunbartonshire, United Kingdom, G81 4DY 收起 <<
NCT01703156 Low Risk Acute Coronary Syndro... 展开 >>me 收起 << Not Applicable Completed - United States, Oklahoma ... 展开 >> Veteran's Affairs Medical Center Oklahoma City, Oklahoma, United States, 73104 收起 <<
NCT01215253 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.69mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL
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]Song Y, Shryock JC, et al. Antagonism by ranolazine of the pro-arrhythmic effects of increasing late INa in guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 2004 Aug;44(2):192-9.

[3]Keating GM. Ranolazine: a review of its use as add-on therapy in patients with chronic stable angina pectoris. Drugs. 2013; 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; 325(3):875‐881

[5]Marciniak TA, Serebruany V. Ranolazine, ACE Inhibitors, and Angiotensin Receptor Blockers. Am J Med. 2019; 132(12):e844‐e845

[6]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; 418(1-2):105‐110

[7]Greiner L, Hurren K, Brenner M. Ranolazine and Its Effects on Hemoglobin A1C. Ann Pharmacother. 2016; 50(5):410‐415