Ranolazine-d8 dihydrochloride(Synonyms: CVT 303-d8 dihydrochloride; RS 43285-d8)

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Ranolazine-d8 dihydrochloride (Synonyms: CVT 303-d8 dihydrochloride; RS 43285-d8)

Ranolazine-d8 (CVT 303-d8) dihydrochloride 是 Ranolazine dihydrochloride 的氘代物。Ranolazine dihydrochloride (CVT 303 dihydrochloride) 是一种抗心绞痛和抗缺血剂，可通过抑制内向钠电流的后期作用 (对 INa 和 IKr 的 IC50 值分别为 6 μM 和 12 μM) 来发挥功效，而不会影响心率或血压。Ranolazine dihydrochloride 还是脂肪酸氧化的部分抑制剂。

Ranolazine-d8 dihydrochloride(Synonyms: CVT 303-d8 dihydrochloride; RS 43285-d8)

Ranolazine-d8 dihydrochloride Chemical Structure

CAS No. : 1219802-60-4

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生物活性

Ranolazine-d8 (CVT 303-d8) dihydrochloride is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) 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)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

508.51

Formula

C24H27D8Cl2N3O4
CAS 号

1219802-60-4
中文名称

盐酸雷诺嗪 d8 (双盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

    [3]. 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. doi: 10.1124/jpet.108.137729. Epub 2008 Mar 5.

    [4]. 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.

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