For research use only. Not for therapeutic Use.
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].
CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC50 of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists[2].
CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantly lower severity of arthritis scores than vehicletreated mice[2].
| Catalog Number | I045279 |
| CAS Number | 312749-73-8 |
| Synonyms | 2-[2-(4-chlorophenoxy)ethylsulfanyl]-1H-benzimidazole |
| Molecular Formula | C15H13ClN2OS |
| Purity | ≥95% |
| InChI | InChI=1S/C15H13ClN2OS/c16-11-5-7-12(8-6-11)19-9-10-20-15-17-13-3-1-2-4-14(13)18-15/h1-8H,9-10H2,(H,17,18) |
| InChIKey | KZEWVENYWPSSOZ-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)NC(=N2)SCCOC3=CC=C(C=C3)Cl |
| Reference | [1]. Munuganti RS, et al. Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives. J Med Chem. 2013;56(3):1136-1148. [2]. Murakoshi M, et al. Discovery and pharmacological effects of a novel GPR142 antagonist. J Recept Signal Transduct Res. 2017;37(3):290-296. |
