BAY-0069

BAY-0069 is a peroxisome proliferator-activated receptor gamma (PPARgamma) inverse agonist. It acts as an inverse agonist in a co-repressor reporter assay with a peptide from nuclear receptor co-repressor 2 (NCOR2, EC50 = 9.6 nM). BAY-0069 selectively induces PPARgamma- over PPARalpha- or PPARdelta-mediated gene transcription in reporter assays using CHO cells (IC50s = 6.3, 7,500, and 9,000 nM for the human receptors, respectively). BAY-0069 inhibits the proliferation of UM-UC-9 human bladder cancer cells that endogenously contain a focal amplification of PPARG, the gene encoding PPARgamma (IC50 = 2.5 nM). In vivo, BAY-0069 (75 mg/kg, i.p.) decreases intratumoral mRNA expression of the PPARgamma target gene FABP4, the gene encoding fatty acid binding protein 4, in a UM-UC-9 mouse xenograft model.Formal Name: 2-bromo-N-[2-(4-ethylphenyl)-5-benzoxazolyl]-5-nitro-benzamide. CAS Number: 420826-65-9. Molecular Formula: C22H16BrN3O4. Formula Weight: 466.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C(C1=CC([N+]([O-])=O)=CC=C1Br)NC2=CC=C3OC(C4=CC=C(CC)C=C4)=NC3=C2. InChi Code: InChI=1S/C22H16BrN3O4/c1-2-13-3-5-14(6-4-13)22-25-19-11-15(7-10-20(19)30-22)24-21(27)17-12-16(26(28)29)8-9-18(17)23/h3-12H,2H2,1H3,(H,24,27). InChi Key: BJSIVXYQIGFUCG-UHFFFAOYSA-N.