Tasimelteon

Catalog No.S4281 Synonyms: BMS 214778, VEC 162

For research use only.

Tasimelteon (BMS 214778, VEC 162) is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).

Tasimelteon Chemical Structure

CAS No. 609799-22-6

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Biological Activity

Description Tasimelteon (BMS 214778, VEC 162) is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).
Targets
MT2 receptor [1]
()
MT1 receptor [1]
()
9.8(pKi) 9.45(pKi)
In vitro

Tasimelteon is a circadian regulator that resets the master clock in the suprachiasmatic nuclei of the hypothalamus by binding to both melatonin MT1 and MT2 receptors making it a dual melatonin receptor agonist[3]. The affinity of tasimelteon for the MT2 receptor is 4-fold higher than its affinity for the MT1 receptor[2].

In vivo In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin[1]. Tasimelteon has a mean absolute bioavailability of approximately 38.3%. The higher oral-to-IV exposure ratios and decrease in the metabolite-to-parent ratios after IV administration for tasimelteon's metabolites indicate that although tasimelteon is subject to first-pass metabolism, a substantial fraction of its metabolism occurs post- rather than presystemically. Both oral and IV tasimelteon were well tolerated[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 49 mg/mL
(199.73 mM)


Chemical Information

Molecular Weight 245.32
Formula

C15H19NO2

CAS No. 609799-22-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(=O)NCC1CC1C2=C3CCOC3=CC=C2

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04652882 Recruiting Drug: Tasimelteon|Drug: Placebo Sleep Wake Disorders|Sleep Disorders Circadian Rhythm|Chronobiology Disorders Vanda Pharmaceuticals December 9 2020 Phase 3
NCT02776215 Unknown status Drug: tasimelteon Circadian Rhythm Sleep Disorders|Non-24 Hour Sleep-Wake Disorder|Autism Spectrum Disorder|Smith-Magenis Syndrome Vanda Pharmaceuticals September 2016 Phase 1
NCT02231008 Unknown status Drug: tasimelteon Smith-Magenis Syndrome|Circadian Vanda Pharmaceuticals September 2015 Phase 2|Phase 3
NCT02130999 Completed Drug: tasimelteon 20 mg capsule|Drug: tasimelteon 2 mg I.V. Non-24-Hour-Sleep-Wake Disorder Vanda Pharmaceuticals May 2014 Phase 4
NCT01637636 Completed Drug: tasimelteon|Drug: Rifampin|Drug: Ketoconazole Healthy Vanda Pharmaceuticals June 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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