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.

Product information

CAS Number: 760944-56-7

Molecular Weight: 497.55

Formula: C24H31N7O5

Chemical Name: {3-[(1S)-1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl]-[1,2,4]triazolo[4,3-a]pyridin-5-yl}methyl N-(carbamoylmethyl)-N-methylcarbamate

Smiles: CN(CC(N)=O)C(=O)OCC1=CC=CC2=NN=C([C@@H](COCC3C=CC=CC=3)NC(=O)C(C)(C)N)N12

InChiKey: HXOYZOFSGAXBOH-GOSISDBHSA-N

InChi: InChI=1S/C24H31N7O5/c1-24(2,26)22(33)27-18(15-35-13-16-8-5-4-6-9-16)21-29-28-20-11-7-10-17(31(20)21)14-36-23(34)30(3)12-19(25)32/h4-11,18H,12-15,26H2,1-3H3,(H2,25,32)(H,27,33)/t18-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BMS-604992 exhibits high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM) for ghrelin receptor.

In Vivo:

BMS-604992 (500 μg/kg; i.p.; 5 minutes) results in a significant increase in gastric emptying compared with vehicle-treated mice. 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. BMS-604992 (300 mg/kg; p.o.; 5~20 minutes) produces a significant difference at the 5 minutes time point. BMS-604992 (500 μg/kg; i.p.; 4 hours) increases food intake approximately 2-fold compared with vehicle-treated controls.

Products are for research use only. Not for human use.