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Merck
모든 사진(1)

Key Documents

SML2030

Sigma-Aldrich

Tasimelteon

≥98% (HPLC)

동의어(들):

(1R, 2R)-N-[2- (2,3-Dihydrobenzofuran-4-yl)cyclopropylmethyl]propanamide, BMS-214778, Hetlioz, MA 1, N-[[(1R,2R)-2-(2,3-Dihydro-4-benzofuranyl)cyclopropyl]methyl]propanamide, VEC-162

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About This Item

실험식(Hill 표기법):
C15H19NO2
CAS Number:
Molecular Weight:
245.32
MDL number:
UNSPSC 코드:
12352200

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

O=C(CC)NC[C@@H]1C[C@H]1C2=C3C(OCC3)=CC=C2

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

생화학적/생리학적 작용

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.

픽토그램

Exclamation markHealth hazard

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

Repr. 2 - STOT SE 3

표적 기관

Central nervous system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Wilbur P Trey Williams et al.
Pharmacotherapy, 36(9), 1028-1041 (2016-08-09)
Circadian rhythm sleep-wake disorders (CRSWDs) are characterized by persistent or recurrent patterns of sleep disturbance related primarily to alterations of the circadian rhythm system or the misalignment between the endogenous circadian rhythm and exogenous factors that affect the timing or
Christian Lavedan et al.
Neuropharmacology, 91, 142-147 (2014-12-24)
Hetlioz(®) (tasimelteon) is the first approved treatment in the United States for Non-24-Hour Sleep-Wake Disorder (Non-24). We present here data on the in vitro binding affinity of tasimelteon for both human melatonin receptors MT1 and MT2, as well as the

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