产品名称

英文名称：Tasimelteon

同义词

SB40737、NSC-157318、Tasimelteon [USAN]、Tasimelteon [USANINN]、CS-5512、Hetlioz、BMS-214778;VEC-162、CHEBI79042、Tasimelteon, >=98% (HPLC)、BMS 214778、N-(((1R,2R)-2-(2,3-dihydrobenzofuran-4-yl)cyclopropyl)methyl)propionamide、AKOS000113311、DB09071、N05CH03、TASIME、他司美琼

产品性质

CAS编号：609799-22-6

分子式：C15H19NO2

分子量：245.322

MDL号：MFCD09033789

PubChem编号：10220503

别名：他司美琼

英文别名：SB40737|NSC-157318|Tasimelteon [USAN]|Tasimelteon [USANINN]|CS-5512|Hetlioz|BMS-214778;VEC-162|CHEBI79042|Tasimelteon, >=98% (HPLC)|BMS 214778|N-(((1R,2R)-2-(2,3-dihydrobenzofuran-4-yl)cyclopropyl)methyl)propionamide|AKOS000113311|DB09071|N05CH03|TASIME

规格或纯度：97%

英文名称：Tasimelteon

生化机理：Tasimelteon is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep-wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light-dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep-wake schedules. The endogenous rhythm of the circadian pacemaker in the suprachiasmatic nuclei (SCN) is typically slightly longer than 24 h and therefore must be synchronized to the 24-hour day, normally by light, but exogenous melatonin can also phase-shift circadian rhythms. Tasimelteon is a selective agonist for the SCN melatonin receptors MT1 and MT2 with greater affinity for the MT2 receptor thought to be more important in mediating circadian rhythm phase-shifting. EC50 values are 0.75 nM for MT1 and 0.1 nM for MT2 measured by inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells expressing human MT1 and MT2.Dual-acting metatonin MT1/MT2 receptor agonist. Binds\xa0MT2 receptor with greater affinity (K i = 0.0692 - 0.17 nM, depending on cell type)\xa0than the MT1 receptor (K i = 0.304-0.35 nM).

应用：Tasimelteon is a selective dual melatonin receptor (MT1/MT2) agonist with 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 CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：有关更多信息，请参阅SDS。有关溶解度，用法和处理的更多建议？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：Tasimelteon是褪黑素MT1和MT2受体激动剂。Tasimelteon is a melatonin MT1 and MT2 receptor agonist.

ALogP：2.2

IUPAC Name：N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide

INCHI：InChI=1S/C15H19NO2/c1-2-15(17)16-9-10-8-13(10)11-4-3-5-14-12(11)6-7-18-14/h3-5,10,13H,2,6-9H2,1H3,(H,16,17)/t10-,13+/m0/s1

InChi Key：PTOIAAWZLUQTIO-GXFFZTMASA-N

Canonical SMILES：CCC(=O)NCC1CC1C2=C3CCOC3=CC=C2

Isomeric SMILES：CCC(=O)NC[C@@H]1C[C@H]1C2=C3CCOC3=CC=C2

PubChem CID：10220503

ChEMBL Ligand：CHEMBL2103822

Wikipedia：Tasimelteon

CAS Registry No.：609799-22-6

DrugCentral Ligand：4820

GPCRdb Ligand：tasimelteon

溶解性：DMSO 2 mg/mL, clear

敏感性：对热敏感

比旋光度：-45° (C=1,CHCl3)

熔点：78°C

象形图：

信号词：Warning

危险声明：H302 Harmful if swallowedH312 Harmful in contact with skinH332 Harmful if inhaled

预防措施声明：P261,P280,P302+P352,P321,P501,P264,P271,P270,P304+P340,P362+P364,P330,P301+P317,P317

产品包装