A PPARγ inverse agonist
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BAY-0069

Item No. 41525

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $72

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    BAY-0069 is a peroxisome proliferator-activated receptor γ (PPARγ) inverse agonist.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Orsi, D.L., Pook, E., Bräuer, N., et al. Discovery and structure-based design of potent covalent PPARγ inverse-agonists BAY-4931 and BAY-0069. J. Med. Chem. 65(21), 14843-14863 (2022).