MCH-1 antagonist 1

MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Signaling Pathways >> GPCR/G Protein >> MCHR1 (GPR24)

Research Areas >> Metabolic Disease

MCH-1:2.6 nM (Ki)

CYP3A4:10 μM (IC50)

MCH-1 antagonist 1 (Compound 1) also inhibits cytochrome P450 3A4 (CYP3A4) with an IC50 of 10 μM[1].

MCH-1 antagonist 1 is administered to male C57BL/6J DIO mice to assess their pharmacokinetic profile. Effect of MCH-1 antagonist 1 (dosed at 30 mg/kg, po) is measured on the body weight of DIO mice with the AUC0-6 h of 14760 h*ng/mL[1].

[1]. Henderson AJ, et al. Tetrahydrocarboline analogs as MCH-1 antagonists. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7024-8.

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