Catalog No.S4281 Synonyms: BMS 214778, VEC 162
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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|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).|
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. The affinity of tasimelteon for the MT2 receptor is 4-fold higher than its affinity for the MT1 receptor.
|In vivo||In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin. 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.|
|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.
|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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