This chemical can be stored In solvent (DMSO) at -80°C for 6 months or at -20°C for 1 month.
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Wichtige Dokumente
SML2030
Tasimelteon
≥98% (HPLC)
Synonym(e):
(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
Empirische Formel (Hill-System):
C15H19NO2
CAS-Nummer:
Molekulargewicht:
245.32
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77
Preise und Verfügbarkeit sind derzeit nicht verfügbar.
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Assay
≥98% (HPLC)
Form
powder
Farbe
white to beige
Löslichkeit
DMSO: 2 mg/mL, clear
Lagertemp.
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
InChIKey
PTOIAAWZLUQTIO-GXFFZTMASA-N
Biochem./physiol. Wirkung
Dual Melatonin Receptor Agonist (DMRA) used to reset circadian rhythm.
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.
Signalwort
Warning
H-Sätze
Gefahreneinstufungen
Repr. 2 - STOT SE 3
Zielorgane
Central nervous system
Lagerklassenschlüssel
11 - Combustible Solids
WGK
WGK 3
Flammpunkt (°F)
Not applicable
Flammpunkt (°C)
Not applicable
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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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