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描述 | Tasimelteon (BMS-214778) is a dual melatonin receptor agonist (DMRA) with 2.1-4.4 times greater affinity for the MT2 receptor than the MT1 receptor, making it a potential circadian regulator for Non-24-Hour Sleep-Wake Disorder (Non-24) [1][2]. |
体外研究 | Tasimelteon (BMS-214778) exhibits significantly higher affinity for the MT2 receptor (Ki=0.0692 nM and Ki=0.17 nM in NIH-3T3 and CHO-K1 cells, respectively) compared to the MT1 receptor (Ki=0.304 nM and Ki=0.35 nM, respectively). It lacks appreciable affinity for over 160 other pharmacologically relevant receptors and several enzymes [1]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00548340 | Primary Insomnia | Phase 3 | Completed | - | - |
NCT00548340 | - | Completed | - | - | |
NCT01402076 | Healthy Volunteers | Phase 1 | Completed | - | United States, Missouri ... 展开 >> Bio-Kinetic Clinical Applications Springfield, Missouri, United States, 65802 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.08mL 0.82mL 0.41mL |
20.38mL 4.08mL 2.04mL |
40.76mL 8.15mL 4.08mL |
CAS号 | 609799-22-6 |
分子式 | C15H19NO2 |
分子量 | 245.317 |
别名 | BMS-214778;VEC-162;BMS214778, BMS-214778, BMS 214778, VEC162, VEC-162, VEC 162, Tasimelteon, Hetlioz;BMS 214778 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 35 mg/mL(142.67 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |