Tasimelteon

Name: Tasimelteon
Brand: Tocris Bioscience
SKU: 7493

Tocris Bioscience, part of Bio-Techne | Catalog # 7493

COA / SDS

Selective dual melatonin receptor (MT1/MT2) agonist

Key Product Details

Description:	Selective dual melatonin receptor (MT₁/MT₂) agonist
Chemical Name:	N-[[(1R,2R)-2-(2,3-Dihydro-4-benzofuranyl)cyclopropyl]methyl]propanamide
Purity:	≥98% (HPLC)
Molecular Weight:	245.32

View Full Technical Details for Tasimelteon

Technical Data
Citations

Biological Activity for Tasimelteon

Tasimelteon is a high affinity and selective dual melatonin receptor (MT₁/MT₂) agonist (K_i values are 0.304 nM and 0.0692 nM, respectively). It has no significant interaction with any other commonly screened receptors or enzyme binding sites. Tasimelteon induces a potent, concentration-dependent inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells stably expressing human MT₁ (EC₅₀ = 0.74 nM) or expressing human MT₂ (EC₅₀ = 0.1 nM) receptors. Tasimelteon is a circadian regulator.

Technical Data for Tasimelteon

M. Wt	245.32
Formula	C₁₅H₁₉NO₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	609799-22-6
PubChem ID	10220503
InChi Key	PTOIAAWZLUQTIO-GXFFZTMASA-N
Smiles	CCC(NC[C@@H]1C[C@H]1C2=C(CCO3)C3=CC=C2)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Tasimelteon

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	24.53	100
	ethanol	24.53	100

Preparing Stock Solutions for Tasimelteon

The following data is based on the product molecular weight 245.32.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.08 mL	20.38 mL	40.76 mL
5 mM	0.82 mL	4.08 mL	8.15 mL
10 mM	0.41 mL	2.04 mL	4.08 mL
50 mM	0.08 mL	0.41 mL	0.82 mL

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References for Tasimelteon

References are publications that support the biological activity of the product.

Vachharajani Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. J.Pharm.Sci. 2003 PMID: 12661062
Lavedan Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology 2015 PMID: 25534555