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Nivasorexant

Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .

Cat. No.: EX-A10364    Purity: >98%
Chemical
Chemical structure of Nivasorexant


For research only, Do not use for Human!

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SynonymsACT-539313
CAS No.1435480-40-2
Purity>98%
FormulaC23H23N7O2
Mol Weight429.4744
ColorWhite to off-white
StateSolid
SolubilitySoluble in DMSO
Shelf Life>3 years if stored properly
StoragePowder -20℃ 3 years, 4℃ 2 years; In solvent -20℃ 1 month;
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  

[1]. Steiner MA, et al. Evaluating the efficacy of the selective orexin 1 receptor antagonist nivasorexant in an animal model of binge-eating disorder. Int J Eat Disord. 2024;57(7):1418-1432.

[2]. Berger B, et al. Effect of nivasorexant (ACT-539313), a selective orexin-1-receptor antagonist, on multiple cytochrome P450 probe substrates in vitro and in vivo using a cocktail approach in healthy subjects. Pharmacol Res Perspect. 2023;11(5):e01143.

CoACoA of Nivasorexant
Smiles:O=C(C1=CC=C(C)C=C1N2N=CC=N2)N3[C@H](CC4=CC=CC(N5N=CC=N5)=C4)COCC3

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