Tasimelteon

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

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