2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. 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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RGH-706

RGH-706 Chemical Structure

CAS No. : 2027497-52-3

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RGH-706 Related Antibodies

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Description

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[1].

In Vitro

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.

RGH-706 Related Antibodies
In Vivo

RGH-706 (0.3-3 mg/kg; p.o.; twice daily; 14-28 days) induces dose-dependent and sustained body weight loss in diet-induced obese C57BL/6 mice[1].

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

Animal Model: C57BL/6 (male, obese, ~45g average body weight, diet-induced obesity model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; twice daily; 14 days (for 0.3,1,3 mg/kg); twice daily; 28 days (for 3 mg/kg)
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.
Clinical Trial
Molecular Weight

462.97

Formula

C26H27ClN4O2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RGH-706 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RGH-7062027497-52-3RGH706RGH 706MCHR1 (GPR24)Melanin concentrating hormone receptor 1obesitydiet-induced obese C57BL/6 micehERG channelmiceVB-Caco-2 cellsMCH1 receptorhMCH2 receptorsprader?willi syndromeliver microsomeshuman MCH1-expressing cellsInhibitorinhibitorinhibit

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