A potent and selective PPARγ antagonist
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T0070907

Item No. 10026

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-chloro-5-nitro-N-4-pyridinyl-benzamide
CAS Number
313516-66-4
Molecular Formula
C12H8ClN3O3
Formula Weight
277.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:4): .2 mg/mlDMSO: 10 mg/ml
λmax
257 nm
SMILES
ClC1=CC=C([N+]([O-])=O)C=C1C(NC2=CC=NC=C2)=O
InChi Code
InChI=1S/C12H8ClN3O3/c13-11-2-1-9(16(18)19)7-10(11)12(17)15-8-3-5-14-6-4-8/h1-7H,(H,14,15,17)
InChi Key
FRPJSHKMZHWJBE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $16

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    5 mg

    $59

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    10 mg

    $98

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    50 mg

    $423

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    Product Description

    The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo.1,2 There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.3,4 However, only a few antagonists have been reported.5 T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J. Med. Chem. 39(3), 665-668 (1996).

    2. Cantello, B.C.C., Cawthorne, M.A., Cottam, G.P., et al. [[ω-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents. J. Med. Chem. 37, 3977-3985 (1994).

    3. Davies, S.S., Pontsler, A.V., Marathe, G.K., et al. Oxidized alkyl phospholipids are specific, high affinity peroxisome proliferator-activated receptor γ ligands and agonists. The Journal of Biological Chemisty 276(19), 16015-16023 (2001).

    4. Maxey, K.M., Hessler, E., MacDonald, J., et al. The nature and composition of 15-deoxy-Δ12,14-PGJ2. Prostaglandins Other Lipid Mediat. 62(1), 15-21 (2000).

    5. Wright, H.M., Clish, C.B., Mikami, T., et al. A synthetic antagonist for the peroxisome proliferator-activated receptor γ inhibits adipocyte differentiation. The Journal of Biological Chemisty 275(3), 1873-1877 (2000).

    6. Lee, G., Elwood, F., McNally, J., et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor γ, functions as an antagonist of biochemical and cellular activities. The Journal of Biological Chemisty 277(22), 19649-19657 (2002).

    Product Citations

    Díaz-Alonso, J., Paraíso-Luna, J., Navarrete, C., et al. VCE-003.2, a novel cannabigerol derivative, enhances neuronal progenitor cell survival and alleviates symptomatology in murine models of Huntington’s disease. Sci. Rep. 6, 29789 (2016).

    Malaviya, A., and Sylvester, P.W. Synergistic antiproliferative effects of combined g-tocotrienol and PPARg antagonist treatment are mediated through PPARg-independent mechanisms in breast cancer cells. PPAR Res. 2014(439146), (2014).