1. Cell Cycle/DNA Damage
    NF-κB
  2. PPAR

GW9662 

Cat. No.: HY-16578 Purity: 99.53%
Data Sheet SDS Handling Instructions

GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM, with ~10 and ~1000-fold functional selectivity in cells against PPARα and PPARδ, respectively.

For research use only. We do not sell to patients.
GW9662 Chemical Structure

GW9662 Chemical Structure

CAS No. : 22978-25-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $60 In-stock
25 mg $95 In-stock
50 mg $120 In-stock
100 mg $220 In-stock
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Customer Review

    GW9662 purchased from MCE. Usage Cited in: Am J Transl Res. 2016 Dec 15;8(12):5169-5186.

    Inhibition of PPARγ by GW9662 attenuates the anti-apoptotic effect of quercetin. Western blot analysis of cleaved caspase-3 in the indicated groups.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM, with ~10 and ~1000-fold functional selectivity in cells against PPARα and PPARδ, respectively.

    IC50 & Target

    IC50: 3.3 nM/32 nM/2 μM (PPARγ/α/δ)[1]

    In Vitro

    GW9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC50s of 8.48±0.27 (IC50=3.3 nM; n=10), 7.49±0.17 (IC50=32 nM; n=9), and 5.69±0.17 (IC50=2000 nM; n=3), respectively. GW9662 has nanomolar IC50 versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW9662 is a potent and selective antagonist of full-length PPARγ[1]. Co-treatment with both 50 μM Rosiglitazone and 10 μM GW9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM rosiglitazone (P=0.001) or 10 μM GW9662 (P=0.01) alone[2].

    In Vivo

    Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group[3]. GW9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat[4].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 3.6143 mL 18.0714 mL 36.1428 mL
    5 mM 0.7229 mL 3.6143 mL 7.2286 mL
    10 mM 0.3614 mL 1.8071 mL 3.6143 mL
    Cell Assay
    [2]

    GW9662 is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

    Cells (MCF7, MDA-MB-231, MDA-MB-468) are plated in 96-well plates at a density of 1×103 cells per well in RPMI medium. After overnight incubation to allow for cell attachment, the medium is removed and replaced with fresh medium containing varying concentrations of Rosiglitazone (1-100 μM), GW9662 (100 nM-50 μM) or solvent (DMSO) alone. MDA-MB-231 cells are also subjected to combinations of Rosiglitazone (10, 50 μM) and GW9662 (1, 10 μM) added simultaneously. The final concentration of DMSO in all cases does not exceed 0.1% and is not found to be cytotoxic in any of the cell lines tested at this concentration. Chemosensitivity is assessed following a continuous 72 h exposure using a standard MTT assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    GW9662 is dissolved in DMSO and stored at −20°C. The aliquot is diluted with PBS to a final concentration of 10% DMSO (Mice)[3].
    GW9662 is dissolved in DMSO and diluted (Rat)[4].

    Mice[3]
    Inbred C57BL/6 (B6, H2b/b), DBA/1J (DBA/1, H2q/q), FVB/NJ (FVB, H2q/q) mice and congenic C.B10-H2b/b/LilMcd (CB10, H2b/b) mice are used. BADGE or GW9662, are administrated by daily intraperitoneal injection at 30 mg/kg for BADGE, or at 1 mg/kg for GW9662, from one day prior to the experiment and continued for up to 2 weeks. In the FVB AA model, some mice are injected with cyclosporine A (CsA, 50 mg/kg/day) starting 1 hour after the LN injection, and continued for 5 days as immunosuppression. At the end of the experiments, the mice are euthanized by CO2 inhalation.
    Rat[4]
    Sixty-two male Wistar rats weighing 215 to 315 g are used in this study. Animals are randomly allocated into 6 groups as follows: (1) I/R group: control, rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=12); (2) I/R LPS group: rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (3) I/R GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=9); (4) I/R LPS+GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (5) Sham group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=12); (6) Sham GW9662 group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered GW9662 (1 mg/kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=7). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    276.68

    Formula

    C₁₃H₉ClN₂O₃

    CAS No.

    22978-25-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    GW9662
    Cat. No.:
    HY-16578
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