1435480-40-2
Chemical Structure
Nivasorexant
Synonym(s): ACT-539313
- No. CAS: 1435480-40-2
- Formula:C23H23N7O2
- Molecular Weight:429.47
InChIKey: GKPHAIOJCHBZCT-HXUWFJFHSA-N
SMILES: O=C(C1=CC=C(C)C=C1N2N=CC=N2)N3[C@H](CC4=CC=CC(N5N=CC=N5)=C4)COCC3
Biological Activity: 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[1][2].
| Referencia número | Nombre del producto | Pureza | Descripciòn | Pricing | |||||||||||||||||||
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Nivasorexant | 99.83% | 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
