For research use only. Not for therapeutic Use.
Firazorexton (TAK-994 free base) is an orally active, brain-permeable orexin type 2 receptor (OX2R) agonist. Firazorexton has the potential to improve narcolepsy like symptoms[1][2].
Firazorexton activates recombinant human OX2R (EC50 value was 19 nM)[1].
Firazorexton (1, 3, 10, 30 mg/kg, oral) exerts a wakeful effect in mice by activating OX2R[1].
Firazorexton (10 mg/kg oral) significantly increases wakefulness time in monkeys, but does not increase OX-A levels in pooled cerebrospinal fluid (CSF)[2].
| Catalog Number | I027483 |
| CAS Number | 2274802-95-6 |
| Synonyms | N-[(2S,3S)-2-[[3-(3,5-difluorophenyl)-2-fluorophenyl]methyl]-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]methanesulfonamide |
| Molecular Formula | C22H25F3N2O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C22H25F3N2O4S/c1-22(2,29)21(28)27-8-7-18(26-32(3,30)31)19(27)11-13-5-4-6-17(20(13)25)14-9-15(23)12-16(24)10-14/h4-6,9-10,12,18-19,26,29H,7-8,11H2,1-3H3/t18-,19-/m0/s1 |
| InChIKey | VOSAWOSMGPKQEQ-OALUTQOASA-N |
| SMILES | CC(C)(C(=O)N1CCC(C1CC2=C(C(=CC=C2)C3=CC(=CC(=C3)F)F)F)NS(=O)(=O)C)O |
| Reference | [1]. Ishikawa T, et al. TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 Receptor-Selective Agonist, Suppresses Fragmentation of Wakefulness and Cataplexy-Like Episodes in Mouse Models of Narcolepsy. J Pharmacol Exp Ther. 2023 Jun;385(3):193-204. [2]. Yamada R, et al. The orexin receptor 2 (OX2R)-selective agonist TAK-994 increases wakefulness without affecting cerebrospinal fluid orexin levels in cynomolgus monkeys. Pharmacol Biochem Behav. 2024 Jan;234:173690. |
