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GSK0660

Chemical Structure : GSK0660

CAS No.: 1014691-61-2

GSK0660 (GSK-0660;GSK 0660)

Catalog No.: PC-43009Not For Human Use, Lab Use Only.

GSK0660 is a potent, selective, dual PPARβ/δ antagonist with pIC50 of 6.8 (160 nM), shows no activity on PPARα and PPARγ (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK0660 is a potent, selective, dual PPARβ/δ antagonist with pIC50 of 6.8 (160 nM), shows no activity on PPARα and PPARγ (IC50>10 uM).
GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.53, reduces CPT1a expression in skeletal muscle cells with EC50 of 100 nM, as well as ANGPTL4 but not PDK4.
GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells.

Physicochemical Properties

M.Wt 418.4866
Formula C19H18N2O5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 49 mg/mL

Chemical Name/SMILES

2-Thiophenecarboxylic acid, 3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-, methyl ester

References

1. Shearer BG, et al. Mol Endocrinol. 2008 Feb;22(2):523-9.

2. Jiménez R, et al. J Pharmacol Exp Ther. 2010 Feb;332(2):554-61.

3. Riahi Y, et al. Diabetes. 2010 Apr;59(4):808-18.

4. Lee WJ, et al. J Cell Biochem. 2018 Feb 1. doi: 10.1002/jcb.26732.

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