Tasimelteon

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Cat.No. 7493 - Tasimelteon | C15H19NO2 | CAS No. 609799-22-6
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)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity for Tasimelteon

Tasimelteon is a high affinity and selective dual melatonin receptor (MT1/MT2) agonist (Ki 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 Data 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.

Select a batch to recalculate based on the batch molecular weight:
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.

Lavedan et al (2015) Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology 91 142 PMID: 25534555

Vachharajani et al (2003) Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. J.Pharm.Sci. 92 760 PMID: 12661062


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Keywords: Tasimelteon, Tasimelteon supplier, Potent, selective, dual, melatonin, receptors, MT1, MT2, agonists, circadian, rhythm, regulators, Melatonin, (MT), Receptors, 7493, Tocris Bioscience

Citations for Tasimelteon

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Literature in this Area

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