312749-73-8

GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR139.1 Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine.2?CLP-3094? (312749-73-8) was identified as a potent and selective GPR142 antagonist with an IC50=2.3 μM against 1 mM L-tryptophan. It inhibited insulin secretion from islets induced by L-tryptophan and other agonists and displayed anti-inflammatory activity in a mouse arthritis model.3

CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].

Susens et al. (2006), Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development, Neuropharmacology, 55 512 Lizarzaburu et al. (2012), Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus; Bioorg. Med. Chem. Lett., 22 5942 Murakoshi et al. (2017), Discovery and pharmacological effects of a novel GPR142 antagonist; Recept. Signal. Transduct. Res., 37 290