| Bioactivity | ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1]. | |||||||||
| Invitro | ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells[1]. | |||||||||
| In Vivo | ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response with no affecting motor or cognitive function in rats[1].ACT-335827 (oral administration, 300 mg/kg, everyday, 4 weeks) has less effect on metabolic syndrome (MetS), such as diet-induced obesity (DIO) in male Wistar rats[2]. Animal Model: | |||||||||
| Name | ACT-335827 | |||||||||
| CAS | 1354039-86-3 | |||||||||
| Formula | C31H38N2O5 | |||||||||
| Molar Mass | 518.64 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Michel A Steiner, et al. Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist. ChemMedChem. 2013 Jun;8(6):898-903. [2]. Michel A Steiner, et al. The selective orexin receptor 1 antagonist ACT-335827 in a rat model of diet-induced obesity associated with metabolic syndrome. Front Pharmacol. 2013 Dec 30;4:165. |
ACT-335827
CAS: 1354039-86-3 F: C31H38N2O5 W: 518.64
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and
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