BMS-604992 free base
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.
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- CAS. Nr.: 760944-56-7
- Formel: C24H31N7O5
- Molecular Weight:497.55
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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TC-G-1008 (Standard)Reference Standard -
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RelamorelinGHSR Agonist -
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JMV 3002 -
HY-14495
BMS-604992GHSR Agonist -
HY-145364
Ghrelin receptor full agonist-2GHSR Agonist -
HY-14495B
BMS-604992 dihydrochlorideGHSR Agonist
Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice
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Dosage:500 μg/kg
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Administration:I.p.; 5 minutes
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Result:Resulted in a significant increase in gastric emptying compared with vehicle-treated mice.
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Animal Model:C57BL/6 mice
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Dosage:1~1000 mg/kg
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Administration:P.o.; 1 hour
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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
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Dosage:300 mg/kg
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Administration:P.o.; 5~20 minutes
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Result:Observed a significant difference at the 5 minutes time point.
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Animal Model:Male GhrR KO and WT mice
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Dosage:500 μg/kg
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Administration:I.p.; 4 hours
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Result:Increased food intake approximately 2-fold compared with vehicle-treated controls.
Chemical Information
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CAS. Nr. 760944-56-7
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Molecular Weight 497.55
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Formel C24H31N7O5
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SMILES
O=C(OCC1=CC=CC2=NN=C([C@H](NC(C(C)(N)C)=O)COCC3=CC=CC=C3)N12)N(CC(N)=O)C
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Synonyms
EX-1314 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BMS-604992 free base Related Classifications
HY-14495A Related Classifications
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