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    GW9662
    GW9662

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0826
    CAS #: 22978-25-2Purity ≥98%

    Description: GW9662 is a novel, potent, irreversible and selective PPAR (peroxisome proliferator-activated receptor) antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 100 to 1000-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ. GW9662 prevented activation of PPARgamma and inhibited growth of human mammary tumour cell lines. GW9662 may permit use of anti-ER strategies to inhibit breast cancer in ER- patients. GW9662 suppresses the cell viability with IC50 values ranging from 20-30μM. 

    References: Biochemistry. 2002 May 28;41(21):6640-50; Kidney Int. 2005 Aug;68(2):529-36.

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    Molecular Weight (MW)276.68
    FormulaC13H9ClN2O3
    CAS No.22978-25-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 55 mg/mL (198.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL
    SynonymsGW-9662; GW 9662; GW9662;  

    Chemical Name: 2-Chloro-5-nitro- N -phenylbenzamide

    InChi Key: DNTSIBUQMRRYIU-UHFFFAOYSA-N

    InChi Code: InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)

    SMILES Code: O=C(NC1=CC=CC=C1)C2=CC([N+]([O-])=O)=CC=C2Cl           


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    In Vitro

    In vitro activity: GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. GW9662 acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. GW9662 prevents activation of PPARγ and inhibits growth of human mammary tumour cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 of 20 μM-30 μM, suggesting either the existence of PPARγ agonistic properties of GW9662 or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with both Rosiglitazone (50 μM) and GW9662 (10 μM) results in statistically lower viable cell numbers after 7 days in MDA-MB-231 cells. PPARγ1 ligands could suppress RANKL-induced osteoclast formation in primary murine myeloid (BMs) and RAW264.7 cells. Importantly, suppression by these ligands is reversed in a concentration-dependent fashion with GW 9662 (2 μM). GW 9662 (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. GW 9662 (1 μM) blocks RANKL activation of NF-κB in RAW264.7 cells. GW9662 (10 μM) inhibits hormone- and agonist-induced adipogenesis of primary preadipocytes from patients with thyroid eye disease.


    Kinase Assay: The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8). 


    Cell Assay: MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing rosiglitazone (50 μM), GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.

    In VivoPretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, GW9662 (1 mg/kg i.p.) abolishes the protective effects of LPS.
    Animal modelMale Wistar rats 
    Formulation & DosageDissolved in 10% (v/v) DMSO; 1 mg/kg; i.p. injection
    References

    Biochemistry. 2002 May 28;41(21):6640-50; Kidney Int. 2005 Aug;68(2):529-36.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GW9662


    Large image of Figure 1.
    Effect of GW9662 on renal/glomerular dysfunction mediated by I/R in rats pretreated with lipopolysaccharide. Kidney Int. 2005 Aug;68(2):529-36.
     

    GW9662

    Large image of Figure 4.
    Effect of GW9662 on reperfusion injury mediated by I/R in rats pretreated with lipopolysaccharide. Kidney Int. 2005 Aug;68(2):529-36.
     

    GW9662

    Large image of Figure 2.
    Effect of GW9662 on tubular dysfunction subsequent to I/R in rats pretreated with lipopolysaccharide.

    Large image of Figure 3.

    GW9662

    Effect of GW9662 on urine flow subsequent to I/R in rats pretreated with lipopolysaccharide. Kidney Int. 2005 Aug;68(2):529-36.


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