Almorexant (Act-078573) |ACT078573|buy from supplier D&C Chemicals

Almorexant (Act-078573) |ACT078573|buy from supplier D&C Chemicals

DC Chemicals supplies: Almorexant (Act-078573) ,cas: 871224-64-5,Catalog: DC7692,In stock.

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Product name: Almorexant (Act-078573) , Synonyms: ACT-078573; ACT 078573; ACT078573, cas: 871224-64-5, MW: 512.56, Molecule Formula: C29H31F3N2O3

Almorexant (Act-078573) , purity: >98%, Best price from D&C Chemicals. Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]

Target: Dual OX!/OX2 receptor

in vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. 

in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].For the detailed information about the solubility of Almorexant(ACT078573)  in water, the solubility of Almorexant(ACT078573)  in DMSO, the solubility of Almorexant(ACT078573)  in PBS buffer, the animal experiment of Almorexant(ACT078573) ,the in vivo and in vitro test of Almorexant(ACT078573) ,the cell experiment of Almorexant(ACT078573) ,the IC50 and EC50 of Almorexant(ACT078573)  please contact DC Chemicals.