Home Neuronal Signaling MT Receptor agonist Tasimelteon For research use only.

Tasimelteon

Synonyms: BMS 214778, VEC 162

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

Tasimelteon Chemical Structure

CAS: 609799-22-6

Selleck's Tasimelteon has been cited by 1 publication

Purity & Quality Control

Batch: S428101 DMSO] 49 mg/mL] false] ] ] false] ] ] false Purity: 99.74%
99.74

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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
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 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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05361707 Recruiting Autism Spectrum Disorder|Sleep Disorder|Neurological Disorder|Sleep Disturbance Vanda Pharmaceuticals July 28 2021 Phase 3
NCT04652882 Unknown status Sleep Wake Disorders|Sleep Disorders Circadian Rhythm|Chronobiology Disorders Vanda Pharmaceuticals December 9 2020 Phase 3
NCT02776215 Unknown status Circadian Rhythm Sleep Disorders|Non-24 Hour Sleep-Wake Disorder|Autism Spectrum Disorder|Smith-Magenis Syndrome Vanda Pharmaceuticals September 2016 Phase 1
NCT02231008 Completed Smith-Magenis Syndrome|Circadian Vanda Pharmaceuticals September 2015 Phase 2|Phase 3
NCT02130999 Completed Non-24-Hour-Sleep-Wake Disorder Vanda Pharmaceuticals May 2014 Phase 4

Chemical lnformation & Solubility

Molecular Weight 245.32 Formula

C15H19NO2
CAS No. 609799-22-6 SDF --
Smiles CCC(=O)NCC1CC1C2=C3CCOC3=CC=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 49 mg/mL ( (199.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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