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

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

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

GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.

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   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
200 mg   Get quote  
500 mg   Get quote  

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Description

GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. IC50 Value: 1 nM(EC50) Target: PPARβ/δ in vitro: GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, GW501516 is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. GW 501516 reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. in vivo: GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. GW501516 induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice.

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
References
M.Wt

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

Purity: 99.26%

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GW 501516
Cat. No.:
HY-10838
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