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

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

Cat. No.: HY-10838 Purity: 99.26%
Data Sheet SDS 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 $55 In-stock
5 mg $50 In-stock
10 mg $78 In-stock
50 mg $190 In-stock
100 mg $260 In-stock
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  • 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].

References
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
[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]

Rat: 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].

Mouse: 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

453.5

Formula

C₂₁H₁₈F₃NO₃S₂

CAS No.

317318-70-0

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.

Purity: 99.26%

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