A PPARγ inverse agonist
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BAY-4931

Item No. 40668

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-chloro-N-[2-(4-ethylphenyl)-5-benzoxazolyl]-5-nitro-benzamide
CAS Number
423150-91-8
Molecular Formula
C22H16ClN3O4
Formula Weight
421.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
ClC1=CC=C(C=C1C(NC2=CC=C3OC(C4=CC=C(CC)C=C4)=NC3=C2)=O)[N+]([O-])=O
InChi Code
InChI=1S/C22H16ClN3O4/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
WFEBALYYDASKIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $165

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    25 mg

    $379

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    Product Description

    BAY-4931 is a 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 = 5.8 nM). BAY-4931 selectively induces PPARγ-mediated gene transcription (IC50 = 0.4 nM for the human receptor) over PPARα- or PPARδ-mediated gene transcription in reporter assays using CHO cells (IC50s = >50 µM for both for the human receptors). BAY-4931 inhibits the proliferation of UM-UC-9 human bladder cancer cells that endogenously contain a focal amplification of PPARG, the gene encoding PPARγ (IC50 = 3.4 nM).

    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).