An OX1R and OX2R dual antagonist (Kis = 2.5 and 0.31 nM

Filorexant – 50 mg

Brand:
Cayman
CAS:
1088991-73-4
Storage:
-20
UN-No:
Non-Hazardous - /

Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).{48849} It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.  

 

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SKU: 29490 - 50 mg Category:

Description

An OX1R and OX2R dual antagonist (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors); selectively inhibits OX1R and OX2R over a panel of >170 receptors and enzymes; inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both); decreases locomotor activity in rats during the dark cycle at 10 mg/kg; reduces the time spent awake and decreases the latency to SWS1 and SWS2, but not REM sleep, in dogs at 0.5 mg/kg; increases the duration of SWS2, but not SWS1 or REM sleep, in the same model

Formal name: [(2R,5R)-5-[[(5-fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]-methanone

Synonyms: 

Molecular weight: 420.5

CAS: 1088991-73-4

Purity: ≥98%

Formulation: A solid

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