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

Tasimelteon-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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

250.35

C₁₅H₁₄D₅NO₂

1962124-51-1

609799-22-6

他司美琼 d₅

Room temperature in continental US; may vary elsewhere.

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

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

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

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