GW 0742

Cat. No. 2229

GW 0742 C21H17F4NO3S2 [317318-84-6]

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Chemical Name: [4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]acetic acid

Biological Activity

Potent and highly selective PPARδ agonist. EC50 values are 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. Neuroprotective in rat cerebellar granule neuronal cultures after brief (12-hour) exposure but exhibits inherent toxicity after prolonged (48-hour) incubation. Increases rate of fatty acid oxidation and protects against ischemia/reperfusion injury in neonatal and adult cardiomyocytes.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
471.49
Formula:
C21H17F4NO3S2
Solubility:
Soluble to 50 mM in ethanol and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
317318-84-6

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 Data Sheet

Certificate of Analysis / Product Datasheet
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Yue et al (2008) In vivo activation of peroxisome proliferator-activayed receptor-δ protects the heart from ischemia/reperfusion injury in Zucker fatty rats. J.Pharm.Exp.Ther. 325 466.

Smith et al (2004) Effect of the peroxisome proliferator-activated receptor β activator GW0742 in rat cultured cerebellar granule neurons. J.Neurosci.Res. 77 240. PMID: 15211590.

Sznaidman et al (2003) Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity. Bioorg.Med.Chem.Lett. 13 1517. PMID: 12699745.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GW 0742 include:

Niu et al (2015) Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Invest Ophthalmol Vis Sci 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.

Perez-Schindler et al (2014) The coactivator PGC-1α regulates skeletal muscle oxidative metabolism independently of the nuclear receptor PPARβ/δ in sedentary mice fed a regular chow diet. Diabetologia 57 2405. PMID: 25116175.

Teske et al (2014) Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs. Drug Des Devel Ther 3. PMID: 25485183.

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

Hatano et al (2010) Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators. PLoS One 125 160. PMID: 19818482.

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Keywords: GW 0742, supplier, selective, potent, PPARδ, PPARdelta, agonists, Peroxisome, Proliferator-activating, Receptors, GW0742, GlaxoSmithKline, GSK, Tocris Bioscience, PPARδ Agonist products

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