CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR) . CLP-3094 inhibits AR transcriptional activity (IC 50 =4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
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Product Description
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC 50 =4 μM). CLP-3094 is a selective, potent GPR142 antagonist .
In Vitro
CLP-3094 inhibits both an increase of intracellular Ca 2+ concentration ([Ca 2+ ]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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)Dosage: 30, 100 mg/kg Administration: I.p. daily from Day 0 to Day 11 Result: Dose-dependently reduced, by not much, the arth-ritis scores.
This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
