Tasimelteon

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tasimelteon (BMS-214778) 是一种具有口服活性，选择性的双重褪黑激素受体激动剂 (DMRA)。Tasimelteon 对 MT2 受体的亲和力是 MT1 受体的 2.1-4.4 倍。Tasimelteon 是一种昼夜节律性调节剂，具有用于非 24 小时睡眠/觉醒障碍 (Non-24) 的潜力。

Tasimelteon (trade name Hetlioz) is a drug approved by the FDA solely for the treatment of non-24-hour sleep?–wake disorder (often designated as N24HSWD) in totally blind adults. It is a selective agonist for the melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, similar to other members of the melatonin receptor agonist class of which ramelteon (2005) and agomelatine (2009) were the first approved.(In Vitro):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.

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.

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BMS214778, VEC162, VEC-162,Tasimelteon, Hetlioz

Angiogenesis

FAK

Melatonin Receptor

Neurological Disease

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609799-22-6

245.32

C15H19NO2

>98% (HPLC)

DMSO : ≥ 33 mg/mL; 134.52 mM

C(=O)(CC)NC[C@H]1[C@@H](C1)c1c2CCOc2ccc1

N-(((1R,2R)-2-(2,3-dihydrobenzofuran-4-yl)cyclopropyl)methyl)propionamide

(-20℃)

With Ice Pack

≥ 2 years