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Biological Activity for GW 0742
GW 0742 is a 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.
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for GW 0742
Technical Data for GW 0742
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GW 0742
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GW 0742
The following data is based on the product molecular weight 471.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.12 mL||10.6 mL||21.21 mL|
|5 mM||0.42 mL||2.12 mL||4.24 mL|
|10 mM||0.21 mL||1.06 mL||2.12 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References for GW 0742
References are publications that support the biological activity of the product.
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
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
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
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Keywords: GW 0742, GW 0742 supplier, selective, potent, PPARδ, PPARdelta, agonists, Peroxisome, Proliferator-activating, Receptors, GW0742, GlaxoSmithKline, GSK, 2229, Tocris Bioscience
14 Citations for GW 0742
Citations are publications that use Tocris products. Selected citations for GW 0742 include:
Batista et al (2012) Structural insights into human peroxisome proliferator activated receptor delta (PPAR-delta) selective ligand binding. PLoS One 7 e33643 PMID: 22606221
Tian et al (2012) PPARδ activation protects endothelial function in diabetic mice. Diabetes 61 3285 PMID: 22933110
Zhang (2017) PPARD is an Inhibitor of Cartilage Growth in External Ears Int J Biol Sci 13 669 PMID: 28539839
Smith et al (2019) Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties. Psychopharmacology (Berl) PMID: 31119329
Wang et al (2017) Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation. J Mol Cell Biol 9 338 PMID: 28992291
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
Halstead et al (2017) Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation. Elife 6 PMID: 29143738
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
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
Martín-Martín et al (2018) PPARδ Elicits Ligand-Independent Repression of Trefoil Factor Family to Limit Prostate Cancer Growth. Cancer Res 78 399 PMID: 29187400
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
Niu et al (2015) Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Invest Ophthalmol Vis Sci 9 5625 PMID: 26508837
Tsai et al (2014) Decrease of PPARδ in Type-1-Like Diabetic Rat for Higher Mortality after Spinal Cord Injury. PPAR Res 2014 456386 PMID: 24817882
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
Do you know of a great paper that uses GW 0742 from Tocris? Please let us know.
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Literature in this Area
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