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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
|Storage||Store at -20°C|
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|
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|
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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