Tasimelteon | BMS-214778 | Dual Melatonin Receptor Agonist

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Tasimelteon/他司美琼 {[allProObj[0].p_purity_real_show]}

货号：A125322 同义名： BMS-214778; VEC-162

Tasimelteon 是一种口服活性的双重褪黑激素受体激动剂，对 MT2 受体的亲和力高于 MT1（2.1–4.4 倍），适用于昼夜节律调控及非 24 小时睡眠/觉醒障碍机制研究。

Tasimelteon/他司美琼化学结构
CAS号：609799-22-6

Tasimelteon/他司美琼 3D分子结构
CAS号：609799-22-6

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Tasimelteon/他司美琼纯度/质量文件产品仅供科研

货号：A125322 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

Tasimelteon/他司美琼生物活性

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].

Tasimelteon/他司美琼临床研究

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 <<

Tasimelteon/他司美琼参考文献

[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/他司美琼实验方案

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

Tasimelteon/他司美琼技术信息

CAS号	609799-22-6
分子式	C₁₅H₁₉NO₂
分子量	245.32
SMILES Code	CCC(NC[C@H]1[C@H](C2=C3CCOC3=CC=C2)C1)=O
MDL No.	MFCD09033789

别名	BMS-214778; VEC-162; BMS214778, BMS-214778, BMS 214778, VEC162, VEC-162, VEC 162, Tasimelteon, Hetlioz
运输	蓝冰
InChI Key	PTOIAAWZLUQTIO-GXFFZTMASA-N
Pubchem ID	10220503

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

临床研究

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 <<
NCT02231008	Smith-Magenis Syndrome ... 展开 >> Circadian 收起 <<	Phase 2 Phase 3	Unknown	-	United States, California ... 展开 >> Santa Monica Clinical Trials Recruiting Santa Monica, California, United States, 90404 Contact: Kerri kcali@smclinicaltrials.com United States, Maryland The Center for Sleep & Wake Disorders Recruiting Chevy Chase, Maryland, United States, 20815 Contact: Jaime sleepdoc@sleepdoc.com United States, Texas Baylor Clinic Recruiting Houston, Texas, United States, 77030 Contact: Zohra Zohra.Huda@bcm.edu 收起 <<
NCT01430754	-		Completed	-	-
NCT01430754	Non-24-Hour Sleep-Wake Disorde... 展开 >>r 收起 <<	Phase 3	Completed	-	-
NCT01428661	-		Completed	-	-
NCT03373201	Jet Lag Type Insomnia	Phase 3	Completed	-	United States, Arkansas ... 展开 >> Vanda Investigational Site Little Rock, Arkansas, United States, 72211 United States, California Vanda Investigational Site Alameda, California, United States, 94501 Vanda Investigational Site San Diego, California, United States, 92103 Vanda Investigational Site Santa Monica, California, United States, 90404 United States, Florida Vanda Investigational Site Oakland Park, Florida, United States, 33334 United States, Georgia Vanda Investigational Site Atlanta, Georgia, United States, 30342 United States, Maryland Vanda Investigational Site Chevy Chase, Maryland, United States, 20815 United States, Missouri Vanda Investigational Site Saint Louis, Missouri, United States, 63141 United States, New York Vanda Investigational Site New York, New York, United States, 10019 United States, Ohio Vanda Investigational Site Cincinnati, Ohio, United States, 45212 United States, Oklahoma Vanda Investigational Site Oklahoma City, Oklahoma, United States, 73112 United States, Texas Vanda Investigational Site Houston, Texas, United States, 77063 收起 <<
NCT01526746	Renal Impairment	Phase 1	Completed	-	United States, Florida ... 展开 >> Clinical Pharmacology of Miami, Inc. Miami, Florida, United States, 33014 Orlando Clinical Research Center Orlando, Florida, United States, 32809 United States, Minnesota DaVita Clinical Research Minneapolis, Minnesota, United States 收起 <<
NCT01637636	Healthy	Phase 1	Completed	-	United States, Missouri ... 展开 >> QPS Bio-Kinetic Clinical Applications Springfield, Missouri, United States, 65802 收起 <<
NCT03291041	Jet Lag Disorder	Phase 2	Completed	-	United States, California ... 展开 >> Vanda Investigational Site Alameda, California, United States, 94501 Vanda Investigational Site Santa Monica, California, United States, 90404 United States, Maryland Vanda Investigational Site Chevy Chase, Maryland, United States, 20815 收起 <<
NCT01428661	Major Depressive Disorder	Phase 2 Phase 3	Completed	-	-
NCT01163032	-		Completed	-	-
NCT01540500	Healthy Volunteers	Phase 1	Completed	-	United States, Missouri ... 展开 >> Bio-Kinetic Clinical Applications Springfield, Missouri, United States, 65802 收起 <<
NCT01477619	Healthy Volunteers	Phase 1	Completed	-	United States, Missouri ... 展开 >> Bio-Kinetic Clinical Applications Springfield, Missouri, United States 收起 <<
NCT01578057	Pharmacodyamics and Pharmacoki... 展开 >>netics of Tasimelteon Alone and in Combination With Ethanol 收起 <<	Phase 1	Completed	-	Canada, Ontario ... 展开 >> INC Research Toronto, Inc. Toronto, Ontario, Canada, M5V 2TC 收起 <<
NCT01429116	Non-24-Hour Sleep-Wake Disorde... 展开 >>r 收起 <<	Phase 3	Completed	-	-
NCT01218789	Non 24 Hour Sleep Wake Disorde... 展开 >>r 收起 <<	Phase 3	Recruiting	December 2018	France ... 展开 >> Recruiting Garches, France Recruiting Lille, France Recruiting Lyon, France Recruiting Montpellier, France Recruiting Paris, France Recruiting Rennes, France Recruiting Toulouse, France 收起 <<
NCT02776215	Circadian Rhythm Sleep Disorde... 展开 >>rs Non-24 Hour Sleep-Wake Disorder Autism Spectrum Disorder Smith-Magenis Syndrome 收起 <<	Phase 1	Recruiting	-	United States, Maryland ... 展开 >> Parexel Early Phase Clinical Unit Recruiting Baltimore, Maryland, United States, 21225 Contact: Amy Roach 667-210-5356 Amy.Roach@parexel.com Principal Investigator: Shannon Marriot 收起 <<
NCT01163032	Non-24-Hour Sleep-Wake Disorde... 展开 >>r 收起 <<	Phase 3	Completed	-	-
NCT01271387	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... 展开 >> Orlando Clinical Research Center Orlando, Florida, United States, 32809 收起 <<
NCT02130999	-		Completed	-	-
NCT02130999	Non-24-Hour-Sleep-Wake Disorde... 展开 >>r 收起 <<	Phase 4	Completed	-	-

Tasimelteon/他司美琼 {[allProObj[0].p_purity_real_show]}

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总药量计算器

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Tasimelteon/他司美琼纯度/质量文件产品仅供科研

Tasimelteon/他司美琼质控信息

Tasimelteon/他司美琼生物活性

Tasimelteon/他司美琼临床研究

Tasimelteon/他司美琼参考文献

Tasimelteon/他司美琼实验方案

Tasimelteon/他司美琼技术信息