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Cat. No. Name Size Price Add Cart
KI3664Act0785735 mg$310

Chemical Characteristic

Product NameAct078573
SynonymsAlMorexant
CAS No.871224-64-5
Molecular Weight 512.56
FormulaC29H31F3N2O3
Chemical Name3,4-Dihydro-6,7-dimethoxy-N-methyl-alpha-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-2(1H)-isoquinolineacetamide
Smiles[C@H]1(N(CCc2cc(c(cc12)OC)OC)C(C(=O)NC)c1ccccc1)CCc1ccc(cc1)C(F)(F)F Cl
Chemical Structure

Biological activities

Almorexant (INN, codenamed ACT-078573) is an orexin antagonist, functioning as a competitive receptor antagonist of the OX1 and OX2 orexin receptors for the treatment of insomnia. The IC50 of Act-078573 to OX1 and OX2 is 6.6 nM and 3.4 nM, respectively [1]. In vitro, Almorexant inhibits the increase of intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat), 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor [2]. In vivo, it can be used by 300 mg/Kg in rats or 100 mg/Kg in dogs [3].

References

[1] Cruz HG, Hoever P, Chakraborty B, et al. Assessment of the abuse liability of a dual orexin receptor antagonist: a crossover study of almorexant and zolpidem in recreational drug users. CNS Drugs. 2014, 28(4):361-372.
[2] Anderson RI, Becker HC, Adams BL, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models. Front Neurosci. 2014, 8:33.
[3] Morairty SR, Wilk AJ, Lincoln WU, et al. The hypocretin/orexin antagonist almorexant promotes sleep without impairment of performance in rats. Front Neurosci. 2014, 8:3.

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Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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