GSK 0660

Cat. No. 3433

GSK 0660 C19H18N2O5S2 [1014691-61-2]

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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

Soluble to 100 mM in DMSO and to 10 mM in ethanol
>99 %
Store at +4°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Bishop-Bailey and Swales (2008) The role of PPARs in the endothelium: Implications for cancer therapy. PPAR Res. 904851.

Shearer et al (2008) Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (NR1C2) antagonist. Mol.Endocrinol. 22 523. PMID: 17975020.

Wang (2008) PPAR-δ in vascular pathophysiology. PPAR Res. 164163. PMID: 19132133.

If you know of a relevant reference for GSK 0660 please let us know.

Citations are publications that use Tocris products. Selected citations for GSK 0660 include:

Lin et al (2015) Development of telmisartan in the therapy of spinal cord injury: pre-clinical study in rats. Invest Ophthalmol Vis Sci 9 4709. PMID: 26316709.

Niu et al (2015) Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Drug Des Devel Ther 9 5625. PMID: 26508837.

Qian et al (2015) Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors. PLoS One 10 e0143439. PMID: 26630504.

Savage et al (2015) RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells. Mol Vis 21 568. PMID: 26015769.

Tsai et al (2014) Merit of ginseng in the treatment of heart failure in type 1-like diabetic rats. Biochem J 2014 484161. PMID: 24745017.

Capozzi et al (2013) Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy. Biomed Res Int 54 4197. PMID: 23716627.

Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. Drug Des Devel Ther 287 25038. PMID: 22685301.

Ramachandran et al (2012) Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer. J Biol Chem 287 38028. PMID: 22992727.

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Keywords: GSK 0660, supplier, Selective, PPARδ, PPARdelta, antagonists, Peroxisome, Proliferator-activating, Receptors, GSK0660, Tocris Bioscience, PPARδ Antagonist products

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