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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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