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Submit ReviewGSK 0660
Description: Selective PPARδ antagonist
Chemical Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester
Purity: ≥99% (HPLC)
Biological Activity for GSK 0660
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.
Compound Libraries for GSK 0660
GSK 0660 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK 0660
| M. Wt | 418.49 |
| Formula | C19H18N2O5S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1014691-61-2 |
| PubChem ID | 46233311 |
| InChI Key | NDFKBGWLUHKMFY-UHFFFAOYSA-N |
| Smiles | O=S(NC1=C(OC)C=C(NC3=CC=CC=C3)C=C1)(C2=C(C(OC)=O)SC=C2)=O |
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 GSK 0660
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.85 | 100 | |
| ethanol | 4.18 | 10 |
Preparing Stock Solutions for GSK 0660
The following data is based on the product molecular weight 418.49. 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 | 2.39 mL | 11.95 mL | 23.9 mL |
| 5 mM | 0.48 mL | 2.39 mL | 4.78 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.39 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets for GSK 0660
References for GSK 0660
References are publications that support the biological activity of the product.
Shearer et al (2008) Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (NR1C2) antagonist. Mol.Endocrinol. 22 523 PMID: 17975020
Wang (2008) PPAR-δ in vascular pathophysiology. PPAR Res. 164163 PMID: 19132133
Bishop-Bailey and Swales (2008) The role of PPARs in the endothelium: Implications for cancer therapy. PPAR Res. 904851 PMID: 19043612
If you know of a relevant reference for GSK 0660, please let us know.
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Keywords: GSK 0660, GSK 0660 supplier, Selective, PPARδ, PPARdelta, antagonists, Peroxisome, Proliferator-activating, Receptors, GSK0660, 3433, Tocris Bioscience
19 Citations for GSK 0660
Citations are publications that use Tocris products. Selected citations for GSK 0660 include:
Niu et al (2015) Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Drug Des Devel Ther 9 5625 PMID: 26508837
Lin et al (2015) Development of telmis. in the therapy of spinal cord injury: pre-clinical study in rats. Invest Ophthalmol Vis Sci 9 4709 PMID: 26316709
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
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
Savage et al (2015) RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells. Mol Vis 21 568 PMID: 26015769
Tsai et al (2014) Merit of ginseng in the treatment of heart failure in type 1-like diabetic rats. Biochem J 2014 484161 PMID: 24745017
Capozzi et al (2013) Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy. Biomed Res Int 54 4197 PMID: 23716627
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
Chen et al (2015) Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets. PLoS One 10 e0127054 PMID: 25970603
Fang et al (2015) Activation of PPAR-δ induces microRNA-100 and decreases the uptake of very low-density lipoprotein in endothelial cells. Br J Pharmacol 172 3728 PMID: 25857370
Castillero et al (2013) PPARβ/δ regulates glucocorticoid- and sepsis-induced FOXO1 activation and muscle wasting. PLoS One 8 e59726 PMID: 23555761
Ramachandran et al (2012) Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer. J Biol Chem 287 38028 PMID: 22992727
Kwonho et al (2019) Activation of peroxisome proliferator-activated receptor delta suppresses BACE1 expression by up-regulating SOCS1 in a JAK2/STAT1-dependent manner. J Neurochem 151 370-385 PMID: 31063584
Kim et al (2014) An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production. Mol Cell Biol 34 4368 PMID: 25312644
Shih et al (2014) Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity. Br J Pharmacol 171 1490 PMID: 24730061
Suarez et al (2014) Modulation of VEGF-induced retinal vascular permeability by peroxisome proliferator-activated receptor-β/δ. Invest Ophthalmol Vis Sci 55 8232 PMID: 25406289
Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. Drug Des Devel Ther 287 25038 PMID: 22685301
Do you know of a great paper that uses GSK 0660 from Tocris? Please let us know.
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