| Identification | Back Directory | [Name]
Carbamic acid, (2-amino-2-oxoethyl)methyl-, [3-[(1S)-1-[(2-amino-2-methyl-1-oxopropyl)amino]-2-(phenylmethoxy)ethyl]-1,2,4-triazolo[4,3-a]pyridin-5-yl]methyl ester (9CI) | [CAS]
760944-56-7 | [Synonyms]
EX-1314 free base
BMS-604992 free base
Carbamic acid, (2-amino-2-oxoethyl)methyl-, [3-[(1S)-1-[(2-amino-2-methyl-1-oxopropyl)amino]-2-(phenylmethoxy)ethyl]-1,2,4-triazolo[4,3-a]pyridin-5-yl]methyl ester (9CI) | [Molecular Formula]
C24H31N7O5 | [MDL Number]
MFCD18782756 | [MOL File]
760944-56-7.mol | [Molecular Weight]
497.55 |
| Hazard Information | Back Directory | [Uses]
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents[1]. | [in vivo]
BMS-604992 (500 μg/kg; i.p.; 5 minutes) results in a significant increase in gastric emptying compared with vehicle-treated mice[1].
BMS-604992 (1~1000 mg/kg; p.o.; 1 hour) Shows a dose-linear increase in plasma concentrations at the 1 hour time point and elicits a dose-responsive increase in food intake relative to vehicle-treated controls, with a minimum effective dose of approximately 10 mg/kg[1].
BMS-604992 (300 mg/kg; p.o.; 5~20 minutes) produces a significant difference at the 5 minutes time point[1].
BMS-604992 (500 μg/kg; i.p.; 4 hours) increases food intake approximately 2-fold compared with vehicle-treated controls[1]. | Animal Model: | C57BL/6 mice | | Dosage: | 500 μg/kg | | Administration: | I.p.; 5 minutes | | Result: | Resulted in a significant increase in gastric emptying compared with vehicle-treated mice.
|
| Animal Model: | C57BL/6 mice | | Dosage: | 1~1000 mg/kg | | Administration: | P.o.; 1 hour | | Result: | Showed a dose-linear increase in plasma concentrations at the 1 hour time point and elicited a dose-responsive increase in food intake relative to vehicle-treated controls, with a minimum effective dose of approximately 10 mg/kg.
|
| Animal Model: | SD rat | | Dosage: | 300 mg/kg | | Administration: | P.o.; 5~20 minutes | | Result: | Observed a significant difference at the 5 minutes time point.
|
| Animal Model: | Male GhrR KO and WT mice | | Dosage: | 500 μg/kg | | Administration: | I.p.; 4 hours | | Result: | Increased food intake approximately 2-fold compared with vehicle-treated controls.
|
| [References]
[1] Charoenthongtrakul S, et, al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009 Jun;329(3):1178-86. DOI:10.1124/jpet.108.150193 |
|
|