CLP-3094 |
| Katalog-Nr.GC62209 |
CLP-3094 ist ein potenter, auf BF3 (Bindungsfunktion 3) gerichteter Inhibitor des Androgenrezeptors (AR).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 312749-73-8
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
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