NGD-4715
NGD-4715 is an orally effective melanin-concentrating hormone receptor 1 (MCHR1) antagonist with IC50 and Ki values of 10.6 nM and 5.9 nM, respectively. NGD-4715 acts as an inhibitor of food intake, a body weight regulator and a metabolic regulator, and reduces food intake, body weight gain and blood glucose levels in diet-induced obese rats. NGD-4715 is applicable to obesity-related research.
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- No. CAS: 873318-96-8
- Fòrmula: C25H30F3N3O3
- Peso molecular:477.52
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
NGD-4715 potently inhibits MCHR, with extremely weak inhibitory activity against hERG channels (IC50 = 38.4 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | CL | Vss | Tmax | Cmax | F | AUC0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 2.1 h | 27.7 mL/min/kg | 2.8 L/kg | 0.5 h | 212 ng/mL | 40.0 % | 765 ng·h/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, obesity-prone, diet-induced obesity model)[1]
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Dosage:5 mg/kg (10-day treatment); 5 mg/kg (26-day treatment); 15 mg/kg (26-day treatment)
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Administration:p.o.; twice daily; 10 days; 26 days
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Result:Caused a 3.1% reduction in body weight over 10 days.
Reduced weight gain relative to controls over 26 days at 5 mg/kg twice daily.
Induced body weight loss over 26 days at 15 mg/kg twice daily.
Dose-dependently reduced daily food intake.
Lowered blood glucose levels, improved glucose tolerance, and reduced diet-induced hyperinsulinemia and hyperleptinemia.
Prevented post-treatment hyperphagia, with body weight gain paralleling vehicle controls during recovery.
Showed no signs of malaise, altered locomotor activity, or anxiogenic effects.
Chemical Information
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No. CAS 873318-96-8
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Peso molecular 477.52
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Fòrmula C25H30F3N3O3
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SMILES
CC1=C(C=CC(OCCO)=C1C)[C@@H]2N3[C@](CCC2)([H])CN(CC3)C(C4=CN=C(C(F)(F)F)C=C4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NGD-4715 Related Classifications
HY-185478 Related Classifications
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