| Bioactivity | Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2]. | ||||||||||||
| Invitro | Tasimelteon (BMS-214778) has 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 CHO-K1 cells, respectively), than for the MT1 receptor (Ki=0.304 nM and Ki=0.35 nM, respectively). Tasimelteon has no appreciable affinity for more than 160 other pharmacologically relevant receptors and several enzymes[1]. | ||||||||||||
| Name | Tasimelteon | ||||||||||||
| CAS | 609799-22-6 | ||||||||||||
| Formula | C15H19NO2 | ||||||||||||
| Molar Mass | 245.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Christian Lavedan, et al. Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7. [2]. Keating GM, et al. Tasimelteon: A Review in Non-24-Hour Sleep-Wake Disorder in Totally Blind Individuals. CNS Drugs. 2016 Mar 22. |
Tasimelteon
CAS: 609799-22-6 F: C15H19NO2 W: 245.32
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4
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