GSK 0660

Catalog # Availability Size / Price Qty
3433/10
3433/50
GSK 0660 | CAS No. 1014691-61-2 | PPAR delta Receptor Inverse Agonists
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Description: Selective PPARδ antagonist

Chemical Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester

Purity: ≥99%

Product Details
Citations (18)
Supplemental Products
Reviews

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:
418.49
Formula:
C19H18N2O5S2
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
1014691-61-2

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.

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.
    Wang
    PPAR Res., 2008;:164163
  3. The role of PPARs in the endothelium: Implications for cancer therapy.
    Bishop-Bailey and Swales
    PPAR Res., 2008;:904851

Product Datasheets

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Citations for GSK 0660

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

18 Citations: Showing 1 - 10

  1. Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties.
    Authors: Smith Et al.
    Psychopharmacology (Berl)  2019;
  2. Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation.
    Authors: Wang Et al.
    J Mol Cell Biol  2017;9:338
  3. Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation.
    Authors: Halstead Et al.
    Elife  2017;6
  4. Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals.
    Authors: Niu Et al.
    Drug Des Devel Ther  2015;9:5625
  5. Development of telmis. in the therapy of spinal cord injury: pre-clinical study in rats.
    Authors: Lin Et al.
    Invest Ophthalmol Vis Sci  2015;9:4709
  6. 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
  7. Activation of PPAR-δ induces microRNA-100 and decreases the uptake of very low-density lipoprotein in endothelial cells.
    Authors: Fang Et al.
    Br J Pharmacol  2015;172:3728
  8. 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
  9. Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets.
    Authors: Chen Et al.
    PLoS One  2015;10:e0127054
  10. Modulation of VEGF-induced retinal vascular permeability by peroxisome proliferator-activated receptor-β/δ.
    Authors: Suarez Et al.
    Invest Ophthalmol Vis Sci  2014;55:8232

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