Tasimelteon

Catalog No.S4281 Synonyms: BMS 214778, VEC 162

Tasimelteon Chemical Structure

Molecular Weight(MW): 245.32

Tasimelteon 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).

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Biological Activity

Description Tasimelteon 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

Solubility (25°C)

In vitro DMSO 49 mg/mL (199.73 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 245.32
Formula

C15H19NO2

CAS No. 609799-22-6
Storage powder
in solvent
Synonyms BMS 214778, VEC 162

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT01540500 Completed Drug: Tasimelteon|Drug: Fluvoxamine Healthy Volunteers Vanda Pharmaceuticals February 2012 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID