RGH-706
RGH-706 is an orally active, blood-brain barrier-permeable, selective MCH1 receptor antagonist with an IC50 of 6.2 nM against hMCHR1. RGH-706 shows no antagonistic activity against hMCH2 receptors. RGH-706 improves obesity. RGH-706 can be used in research related to obesity and Prader-Willi syndrome.
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- CAS No.: 2027497-52-3
- Formule: C26H27ClN4O2
- Masse moléculaire:462.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
RGH-706 (60 min) is a potent MCHR1 antagonist in human MCH1-expressing cells, with an IC50 of 6.2 nM[1].
RGH-706 (3 μM; 5.5 h) has high plasma protein binding (fu = 0.0235) and high brain tissue binding (fu = 0.009) in mouse samples at 3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, obese, ~45g average body weight, diet-induced obesity model)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; twice daily; 14 days (for 0.3,1,3 mg/kg); twice daily; 28 days (for 3 mg/kg)
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Result:Induced dose-dependent body weight loss after 14 days of treatment, with control-subtracted body weight loss of 13.1% at 3 mg/kg b.i.d.
Caused a sustained 10-30% decrease in daily food intake.
Determined an ED50 (dose for 5% weight loss) of 0.25 mg/kg p.o.
Sustained body weight loss with no habituation to treatment in a 28-day DIO study with 3 mg/kg b.i.d.
dosing.
Showed supraproportional increases in plasma and brain concentrations across the 0.3-3 mg/kg dose range: at 0.3 mg/kg, Cmax plasma was 0.175 μM and Cmax brain was 0.258 μM; at 1 mg/kg, Cmax plasma was 0.664 μM and Cmax brain was 1.010 μM; at 3 mg/kg, Cmax plasma was 2.51 μM and Cmax brain was 3.010 μM.
Achieved receptor occupancy of 24% at 0.3 mg/kg b.i.d.
and 99% at 3 mg/kg b.i.d., with corresponding Cu brain/IC50 potency ratios of 0.37 and 5.78, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2027497-52-3
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Masse moléculaire 462.97
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Formule C26H27ClN4O2
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SMILES
O=C1C=C(OCC2=NC=C(Cl)C=C2)C=CN1C3=CC4=C(N(CCN(C(C)C)CC5)C5=C4)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RGH-706 Related Classifications
HY-181551 Related Classifications
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