research use only

Tasimelteon MT Receptor agonist

Name: Tasimelteon
Brand: Selleck Chemicals
SKU: S4281
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4281

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).

Chemical Structure

Molecular Weight: 245.32

Jump to

Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.74

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other MT Receptor Products	Melatonin Luzindole

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (8.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	245.32	Formula	C₁₅H₁₉NO₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	609799-22-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BMS 214778, VEC 162			Smiles	CCC(=O)NCC1CC1C2=C3CCOC3=CC=C2

Mechanism of Action

Targets/IC₅₀/Ki	MT2 receptor 9.8(pKi) MT1 receptor 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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21548834/ [2] https://pubmed.ncbi.nlm.nih.gov/25658956/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4418347/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	Recruiting	Sleep Wake Disorders\|Sleep Disorders Circadian Rhythm\|Chronobiology Disorders	Vanda Pharmaceuticals	December 9 2020	Phase 3
NCT02776215	Completed	Circadian Rhythm Sleep Disorders\|Non-24 Hour Sleep-Wake Disorder\|Autism Spectrum Disorder\|Smith-Magenis Syndrome	Vanda Pharmaceuticals	October 4 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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):