Home / PPAR delta Receptor Inverse Agonists / GSK 0660

GSK 0660

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

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

Purity: ≥99%

Product Details
Citations (19)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

GSK 0660 is a 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. The triggering receptor expressed on myeloid cells 2 inhibits complement component 1q effector mechanisms and exerts detrimental effects during pneumococcal pneumonia.
    Sharif O, Gawish R, Warszawska J, Martins R, Lakovits K, Hladik A, Doninger B, Brunner J, Korosec A, Schwarzenbacher R, Berg T, Kralovics R, Colinge J, Mesteri I, Gilfillan S, Salmaggi A, Verschoor A, Colonna M, Knapp S
    PLoS Pathog, 2014;10(6):e1004167.
  2. Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (NR1C2) antagonist.
    Shearer et al.
    Mol.Endocrinol., 2008;22:523
  3. PPAR-δ in vascular pathophysiology.
    Wang
    PPAR Res., 2008;:164163

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:

19 Citations: Showing 1 - 10

  1. Activation of peroxisome proliferator-activated receptor delta suppresses BACE1 expression by up-regulating SOCS1 in a JAK2/STAT1-dependent manner.
    Authors: Kwonho Et al.
    J Neurochem  2019;151:370-385
  2. 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;
  3. Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation.
    Authors: Wang Et al.
    J Mol Cell Biol  2017;9:338
  4. Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation.
    Authors: Halstead Et al.
    Elife  2017;6
  5. Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals.
    Authors: Niu Et al.
    Drug Des Devel Ther  2015;9:5625
  6. 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
  7. 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
  8. 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
  9. 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
  10. Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets.
    Authors: Chen Et al.
    PLoS One  2015;10:e0127054
  11. 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
  12. An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production.
    Authors: Kim Et al.
    Mol Cell Biol  2014;34:4368
  13. Merit of ginseng in the treatment of heart failure in type 1-like diabetic rats.
    Authors: Tsai Et al.
    Biochem J  2014;2014:484161
  14. 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
  15. Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity.
    Authors: Shih Et al.
    Br J Pharmacol  2014;171:1490
  16. PPARβ/δ regulates glucocorticoid- and sepsis-induced FOXO1 activation and muscle wasting.
    Authors: Castillero Et al.
    PLoS One  2013;8:e59726
  17. Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy.
    Authors: Capozzi Et al.
    Biomed Res Int  2013;54:4197
  18. Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer.
    Authors: Ramachandran Et al.
    J Biol Chem  2012;287:38028
  19. Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply.
    Authors: Mottillo Et al.
    Drug Des Devel Ther  2012;287:25038

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