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T0070907

Item № 10026
CAS № 313516-66-4
Purity ≥98%
product image
                (CAS 313516-66-4)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $9.00 0.00
     5 mg $41.00 0.00
     10 mg $72.00 0.00
     50 mg $315.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

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

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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
A crystalline solid
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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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, 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, 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 Mediators 62, 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, 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

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 Research 2014(439146), (2014).

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