GSK 0660

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Cat.No. 3433 - GSK 0660 | C19H18N2O5S2 | CAS No. 1014691-61-2
Description: Selective PPARδ antagonist
Chemical Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Literature

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.

Compound Libraries

GSK 0660 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.85 100
ethanol 4.18 10

Preparing Stock Solutions

The following data is based on the product molecular weight 418.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

References

References are publications that support the products' biological activity.

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:


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Keywords: GSK 0660, supplier, Selective, PPARδ, PPARdelta, antagonists, Peroxisome, Proliferator-activating, Receptors, GSK0660, PPARdelta, Receptors, PPARdelta, Receptors, Tocris Bioscience

8 Citations for GSK 0660

Citations are publications that use Tocris products. Selected citations for GSK 0660 include:

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

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 telmisartan in the therapy of spinal cord injury: pre-clinical study in rats. Invest Ophthalmol Vis Sci 9 4709 PMID: 26316709

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

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

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


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Reviews

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Literature in this Area

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Nuclear Receptors

Nuclear Receptors Product Listing

A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

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Pathways for GSK 0660

Protocols

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