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| | 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) Basic information |
| Product 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) | | Synonyms: | 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);BMS-604992 free base;EX-1314 free base | | CAS: | 760944-56-7 | | MF: | C24H31N7O5 | | MW: | 497.55 | | EINECS: | | | Product Categories: | | | Mol File: | 760944-56-7.mol | ![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) Structure](CAS/20210305/GIF/760944-56-7.gif) |
| | 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) Chemical Properties |
| density | 1.34±0.1 g/cm3(Predicted) | | pka | 15.23±0.46(Predicted) |
| | 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) Usage And Synthesis |
| 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.
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| 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.
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| 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.
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| 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.
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| | 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 |
| | 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) Preparation Products And Raw materials |
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