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  3. GW 501516

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

Cat. No.: HY-10838 Purity: 99.27%
COA Handling Instructions

GW 501516 (GW 1516) 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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GW 501516 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 28;9:648.  [Abstract]

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

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review


    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM[1].

    IC50 & Target[1]


    1.1 nM (EC50)

    In Vitro

    GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ 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].

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

    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].

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

    Clinical Trial
    Molecular Weight




    CAS No.



    White to off-white




    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (220.51 mM)

    *"≥" means soluble, but saturation unknown.

    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.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.51 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.27%

    Cell Assay

    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

    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.

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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