1039825-68-7

1039825-68-7 structure

Name: MCH-1 antagonist 1
Chemical Name: 4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one
CAS Number: 1039825-68-7
Molecular Formula: C₂₅H₂₆N₄O₂
Molecular Weight: 414.50000
Catalog: Signaling Pathways GPCR/G Protein MCHR1 (GPR24)
Create Date: 2018-05-25 03:46:51
Modify Date: 2024-01-02 11:14:19
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.

Name	4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one
Synonyms	MCH-1 antagonist 1

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Signaling Pathways >> GPCR/G Protein >> MCHR1 (GPR24) Research Areas >> Metabolic Disease
Target	MCH-1:2.6 nM (Ki) CYP3A4:10 μM (IC50)
In Vitro	MCH-1 antagonist 1 (Compound 1) also inhibits cytochrome P450 3A4 (CYP3A4) with an IC50 of 10 μM[1].
In Vivo	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].
References	[1]. Henderson AJ, et al. Tetrahydrocarboline analogs as MCH-1 antagonists. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7024-8.