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.
Acta Pharmacol Sin. 2020 Mar;41(3):373-382.
J Cell Mol Med. 2020 Jun;24(12):6833-6845.
Seizure-induced impairment in neuronal ketogenesis: Role of zinc-α2-glycoprotein in mitochondria
GW9662 purchased from AbMole
Life Sci. 2019 Dec 1;238:116979.
Effects of progesterone on glucose uptake in neurons of Alzheimer's disease animals and cell models.
GW9662 purchased from AbMole
|Source||J Cell Mol Med (2020 Jun). Figure 2. Pioglitazone (Abmole Bioscience, Houston, TX, USA)|
|Incubation Time||24 hours|
|Results||Compared to the DMSO group, a 24-hour treatment with pioglitazone increased the levels of the ZAG protein (1.013 ± 0.135 vs 0.654 ± 0.090, P = 0.004, n = 4) and AZGP1 mRNA (1.474 ± 0.078 vs 1, P = 0.003, n = 3) (Figure 2B,C), while GW9662 significantly decreased the levels of the ZAG protein (0.361 ± 0.097 vs 0.654 ± 0.090, P = 0.013, n = 4) and AZGP1 mRNA (0.482 ± 0.153 vs 1, P = 0.002, n = 3) (Figure 2B,C).|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 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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