For research use only.
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|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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