1. Cell Cycle/DNA Damage
  2. PPAR

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
5 mg USD 60 In-stock
10 mg USD 94 In-stock
50 mg USD 228 In-stock
100 mg USD 312 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


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].

Preparing Stock Solutions
Concentration Volume 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.
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.

Molecular Weight








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

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.

Purity: 99.26%

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