GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM, with at least 100 to 1000-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
|Source||Oncol Lett (2018). Figure 5. GW9662|
|Cell Lines||EC109 cells|
|Incubation Time||72 h|
|Results||GW9662 treatment attenuated the inhibitory effects of carotenoids on EC109 cell viability and the increase in PPARγ protein levels induced by carotenoids was reduced with GW9662 pre.treatment in EC109 cells.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion.
Collino M, et al. Kidney Int. 2005 Aug;68(2):529-36. PMID: 16014029.
GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation.
Seargent JM, et al. Br J Pharmacol. 2004 Dec;143(8):933-7. PMID: 15533890.
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.
Leesnitzer LM, et al. Biochemistry. 2002 May 28;41(21):6640-50. PMID: 12022867.
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