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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); 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; 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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