-CLP 3094
GPR142 antagonist / GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR1391. Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine2. CLP-3094 was identified as a potent and selective GPR142 antagonist with an IC50=2.3 uM 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
Biochemicals & reagents
312749-73-8
1) 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 2) 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 3) Murakoshi et al. (2017), Discovery and pharmacological effects of a novel GPR142 antagonist; J. Recept. Signal. Transduct. Res., 37 290
-20°C
TARGET: GPCR -- RESEARCH AREA: Immunology -- DISEASE AREA: Diabetes; Inflammation