BI 186908

BI 186908 is a selective and orally active MCH receptor 1 antagonist with an IC50 of 22 nM and a Ki of 14 nM. BI 186908 binds with comparably high affinity to the recombinant human, cynomolgus monkey (IC50 of 18 nM), dog (IC50 of 23 nM) and rat (IC50 of 18 nM) MCH-R1. BI 186908 can significantly reduce the body weight of diet-induced obese rats. BI 186908 can be used for the study of obesity[1].

Product Specifications

CAS Number

[1453500-36-1]

UNSPSC

12352005

Target

MCHR1 (GPR24)

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Neurological Disease; Metabolic Disease

Smiles

O=C1C=C(OCC2=NC=C(OC)C=C2)C=NN1CC(C3=CC=C(CN(C)C)C=C3C)=O

Molecular Formula

C23H26N4O4

Molecular Weight

422.48

References & Citations

[1]Thorsten Oost, et al. Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908. Bioorg Med Chem Lett. 2015 Aug 15;25 (16) :3275-80.