Catalog Number: 3433
Chemical Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester
Biological Activity
Selective PPARδ antagonist (IC50 values are 0.155, > 10 and 10 μM at PPARδ, PPARα and PPARγ respectively). Exhibits inverse agonist effects when administered by itself.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (NR1C2) antagonist.
    Shearer et al.
    Mol.Endocrinol., 2008;22:523
  2. PPAR-δ in vascular pathophysiology.
    PPAR Res., 2008;:164163
  3. The role of PPARs in the endothelium: Implications for cancer therapy.
    Bishop-Bailey and Swales
    PPAR Res., 2008;:904851

The citations listed below are publications that use Tocris products. Selected citations for GSK 0660 include:

8 Citations: Showing 1 - 8
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  1. Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals.
    Authors: Niu Et al.
    Drug Des Devel Ther 2015;9:5625
  2. Development of telmisartan in the therapy of spinal cord injury: pre-clinical study in rats.
    Authors: Lin Et al.
    Invest Ophthalmol Vis Sci 2015;9:4709
  3. RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells.
    Authors: Savage Et al.
    Mol Vis 2015;21:568
  4. Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors.
    Authors: Qian Et al.
    PLoS One 2015;10:e0143439
  5. Merit of ginseng in the treatment of heart failure in type 1-like diabetic rats.
    Authors: Tsai Et al.
    Biochem J 2014;2014:484161
  6. Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy.
    Authors: Capozzi Et al.
    Biomed Res Int 2013;54:4197
  7. Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer.
    Authors: Ramachandran Et al.
    J Biol Chem 2012;287:38028
  8. Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply.
    Authors: Mottillo Et al.
    Drug Des Devel Ther 2012;287:25038

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