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GW9662

Cat. No. M2748
GW9662 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 46  USD46 In stock
10mg USD 68  USD68 In stock
25mg USD 108  USD108 In stock
50mg USD 140  USD140 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source J Cell Mol Med (2020 Jun). Figure 2. Pioglitazone (Abmole Bioscience, Houston, TX, USA)
Method drug treatments
Cell Lines Neurons
Concentrations -
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
Method western blotting
Cell Lines EC109 cells
Concentrations 40 μM
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 276.68
Formula C13H9ClN2O3
CAS Number 22978-25-2
Purity 99.55%
Solubility DMSO ≥ 40 mg/mL
Storage at -20°C
References

[1] Collino M, et al. Kidney Int. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion.

[2] Seargent JM, et al. Br J Pharmacol. 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.

[3] Leesnitzer LM, et al. Biochemistry. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GW9662 supplier, PPAR, inhibitors

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