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GW 0742

2229 10 Citations Datasheet / COA / SDS
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2229/50
Cat.No. 2229 - GW 0742 | C21H17F4NO3S2 | CAS No. 317318-84-6
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Description: Highly selective, potent PPARδ agonist

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

Purity: ≥98%

Product Details
Citations (10)
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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.

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity.
    Sznaidman et al.
    Bioorg.Med.Chem.Lett., 2003;13:1517
  2. Effect of the peroxisome proliferator-activated receptor β activator GW0742 in rat cultured cerebellar granule neurons.
    Smith et al.
    J.Neurosci.Res., 2004;77:240
  3. In vivo activation of peroxisome proliferator-activayed receptor-δ protects the heart from ischemia/reperfusion injury in Zucker fatty rats.
    Yue et al.
    J.Pharm.Exp.Ther., 2008;325:466

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Citations for GW 0742

The citations listed below are publications that use Tocris products. Selected citations for GW 0742 include:

10 Citations: Showing 1 - 10

  1. PPARD is an Inhibitor of Cartilage Growth in External Ears
    Authors: Zhang
    Int J Biol Sci  2017;13(5):669
  2. Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals.
    Authors: Niu Et al.
    Invest Ophthalmol Vis Sci  2015;9:5625
  3. 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
  4. The coactivator PGC-1α regulates skeletal muscle oxidative metabolism independently of the nuclear receptor PPARβ/δ in sedentary mice fed a regular chow diet.
    Authors: Perez-Schindler Et al.
    Diabetologia  2014;57:2405
  5. Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs.
    Authors: Teske Et al.
    Drug Des Devel Ther  2014;3
  6. Decrease of PPARδ in Type-1-Like Diabetic Rat for Higher Mortality after Spinal Cord Injury.
    Authors: Tsai Et al.
    PPAR Res  2014;2014:456386
  7. Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy.
    Authors: Capozzi Et al.
    J Allergy Clin Immunol  2013;54:4197
  8. Structural insights into human peroxisome proliferator activated receptor delta (PPAR-delta) selective ligand binding.
    Authors: Batista Et al.
    PLoS One  2012;7:e33643
  9. PPARδ activation protects endothelial function in diabetic mice.
    Authors: Tian Et al.
    Diabetes  2012;61:3285
  10. Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators.
    Authors: Hatano Et al.
    PLoS One  2010;125:160

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VersaClone cDNA Plasmids

Human PPAR delta/NR1C2 (NP_006229) VersaClone cDNA

RDC2078

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