1. GPCR/G Protein
  2. GHSR
  3. BMS-604992 dihydrochloride

BMS-604992 dihydrochloride (Synonyms: EX-1314 dihydrochloride)

Cat. No.: HY-14495B
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BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents.

For research use only. We do not sell to patients.

BMS-604992 dihydrochloride Chemical Structure

BMS-604992 dihydrochloride Chemical Structure

CAS No. : 1469750-46-6

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Description

BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents[1].

IC50 & Target

EC50: 0.4 nM (GHSR), Ki: 2.3 nM (GHSR)[1]

In Vitro

BMS-604992 exhibits high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM) for ghrelin receptor[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

570.47

Formula

C₂₄H₃₃Cl₂N₇O₅

CAS No.
SMILES

O=C(OCC1=CC=CC2=NN=C([[email protected]](NC(C(C)(N)C)=O)COCC3=CC=CC=C3)N12)N(CC(N)=O)C.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BMS-604992EX-1314BMS604992BMS 604992EX1314EX 1314GHSRGrowth hormone secretagogue receptorgrowthhormonesecretagoguefoodintakegastricemptyingsmallintestinaltransitfecaloutputInhibitorinhibitorinhibit

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BMS-604992 dihydrochloride
Cat. No.:
HY-14495B
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