CLP-3094

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.