Formulation: A solid
Formal Name: 2-bromo-N-[2-(4-ethylphenyl)-5-benzoxazolyl]-5-nitro-benzamide
Purity: ≥98%
Formula Markup: C22H16BrN3O4
Formula Weight: 466,3
Shelf life (days): 1460
CAS Number: 420826-65-9
Notes: BAY-0069 is a peroxisome proliferator-activated receptor γ (PPARγ) inverse agonist.{68744} 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 PPARγ- over PPARα- or PPARδ-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 PPARγ (IC50 = 2.5 nM). In vivo, BAY-0069 (75 mg/kg, i.p.) decreases intratumoral mRNA expression of the PPARγ target gene FABP4, the gene encoding fatty acid binding protein 4, in a UM-UC-9 mouse xenograft model.
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