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GW 501516 (Synonyms: GW 1516; GSK-516)

Cat. No.: HY-10838 Purity: 99.26%
Handling Instructions

GW 501516 is a PPARδ agonist with an EC50 of 1.1 nM.

For research use only. We do not sell to patients.

GW 501516 Chemical Structure

GW 501516 Chemical Structure

CAS No. : 317318-70-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 94 In-stock
Estimated Time of Arrival: December 31
50 mg USD 228 In-stock
Estimated Time of Arrival: December 31
100 mg USD 312 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    GW 501516 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 28;9:648.

    Western blot analysis of the protein expression of caspase and Bcl-2 family members in response to GW501516.

    View All PPAR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GW 501516 is a PPARδ agonist with an EC50 of 1.1 nM.

    IC50 & Target

    EC50: 1.1 nM (PPARδ)[1]

    In Vitro

    GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3].

    In Vivo

    GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats[2]. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model[3]. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice[4].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2051 mL 11.0254 mL 22.0507 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 mL
    10 mM 0.2205 mL 1.1025 mL 2.2051 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      GW 501516 is prepared in vehicle control (saline containing 0.5% DMSO)[5].

    References
    Cell Assay
    [3]

    GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body[2].

    Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    453.50

    Formula

    C₂₁H₁₈F₃NO₃S₂

    CAS No.

    317318-70-0

    SMILES

    OC(COC1=CC=C(C=C1C)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)=O

    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

    Purity: 99.26%

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    Product Name:
    GW 501516
    Cat. No.:
    HY-10838
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    GW 501516

    Cat. No.: HY-10838