Powder: -20°C for 3 years | In solvent: -80°C for 2 years
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.
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5 mg | Inquiry | $ 970.00 |
Description | BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents. |
Targets&IC50 | GHSR:0.4 nM (EC50), GHSR:Ki: 2.3 nM |
In vitro | BMS-604992 exhibits high-affinity binding (K i =2.3 nM) and potent functional activity (EC 50 =0.4 nM) for ghrelin receptor[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. |
Synonyms | EX-1314 free base |
Molecular Weight | 497.556 |
Formula | C24H31N7O5 |
CAS No. | 760944-56-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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BMS-604992 free base 760944-56-7 EX-1314 free base BMS 604992 free base BMS604992 free base inhibitor inhibit