GSK0660 - CAS 1014691-61-2
Catalog number:
1014691-61-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H18N2O5S2
Molecular Weight:
418.48
COA:
Inquire
Targets:
PPAR
Description:
GSK0660 is a selective PPARδ antagonist. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10, and it may block TNFα-induced retinal leukostasis.
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Purity:
96%
Appearance:
Solid powder
Synonyms:
GSK0660; GSK-0660; GSK 0660.
Solubility:
Soluble in DMSO, not in water
Storage:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years if stored properly
Canonical SMILES:
O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC
1.Endothelium-dependent vasodilator effects of peroxisome proliferator-activated receptor beta agonists via the phosphatidyl-inositol-3 kinase-Akt pathway.
Jiménez R1, Sánchez M, Zarzuelo MJ, Romero M, Quintela AM, López-Sepúlveda R, Galindo P, Gómez-Guzmán M, Haro JM, Zarzuelo A, Pérez-Vizcaíno F, Duarte J. J Pharmacol Exp Ther. 2010 Feb;332(2):554-61. doi: 10.1124/jpet.109.159806. Epub 2009 Nov 11.
Peroxisome proliferator-activated receptor beta/delta (PPAR-beta) is a ligand-activated transcription factor belonging to the nuclear hormone receptor superfamily that regulates the transcription of many target genes. More recently, acute, nongenomic effects of PPAR-beta agonists have also been described. In the present study, we hypothesized that PPAR-beta agonists might exert acute nongenomic effects on vascular tone. Here, we report that the structurally unrelated PPAR-beta ligands [4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]acetic acid (L-165041) and 4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl] methyl]thio]-2-methylphenoxy]acetic acid (GW0742) induced vascular relaxation in phenylephrine-precontracted endothelium-intact rat aortic rings, which was significantly inhibited by endothelial denudation or nitric-oxide synthase (NOS) inhibition with N(G)-nitro-l-arginine methylester. These relaxant effects reached steady state within 15 min.
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CAS 1014691-61-2 GSK0660

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