2-([2-(4-Chlorophenoxy)ethyl]thio)-1H-benzimidazole

Description

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.2CLP-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

Uses

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].

in vivo

References

[1] UTE SÜSENS. Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development[J]. Neuropharmacology, 2006, 50 4: Pages 512-520. DOI:10.1016/j.neuropharm.2005.11.003
[2] MIKE LIZARZABURU . Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus[J]. Bioorganic & Medicinal Chemistry Letters, 2012, 22 18: Pages 5942-5947. DOI:10.1016/j.bmcl.2012.07.063
[3] MICHIKO MURAKOSHI. Discovery and pharmacological effects of a novel GPR142 antagonist[J]. Journal of Receptors and Signal Transduction, 2017, 87 1: 290-296. DOI:10.1080/10799893.2016.1247861