Tasimelteon-d5(Synonyms: BMS-214778-d5; VEC-162-d5)

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Tasimelteon-d5 (Synonyms: BMS-214778-d5; VEC-162-d5)

Tasimelteon-d5 (BMS-214778-d5) 是 Tasimelteon 的氘代物。Tasimelteon (BMS-214778) 是一种具有口服活性,选择性的双重褪黑激素受体激动剂 (DMRA)。Tasimelteon 对 MT2 受体的亲和力是 MT1 受体的 2.1-4.4 倍。Tasimelteon 是一种昼夜节律性调节剂,具有用于非 24 小时睡眠/觉醒障碍 (Non-24) 的潜力。

Tasimelteon-d5(Synonyms: BMS-214778-d5;  VEC-162-d5)

Tasimelteon-d5 Chemical Structure

CAS No. : 1962124-51-1

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生物活性

Tasimelteon-d5 (BMS-214778-d5) is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].

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

250.35

Formula

C15H14D5NO2

CAS 号

1962124-51-1

中文名称

他司美琼 d5

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]. Christian Lavedan, et al. Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7.

    [3]. Keating GM, et al. Tasimelteon: A Review in Non-24-Hour Sleep-Wake Disorder in Totally Blind Individuals. CNS Drugs. 2016 Mar 22.

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