Cardarine (GW501516)

Catalog No.S5615 Synonyms: Cardarine, GW1516

Cardarine (GW501516) Chemical Structure

Molecular Weight(MW): 453.50

GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.

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Description GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
Targets
PPARδ [1]
(Cell-free assay)
1 nM(Ki)
In vitro

GW501516, a potent agonist to PPARδ, modulates glyco-metabolism, fatty acid metabolism and alleviates insulin resistance. GW501516 increases fatty acid oxidation by increasing the levels of hepatic mRNAs associated with fatty acid β-oxidation, such as acyl-CoA oxidase (ACOX), carnitine palmitoyltransferase-1 (CPT-1) and liver fatty acid binding protein (L-FABP). In skeletal muscle cells, treatment with GW501516 has been shown to prevent fatty acid-induced inflammation and insulin resistance in by preventing the phosphorylation of insulin receptor substrate-1 at Ser307 and the inhibition of insulin-stimulated Akt phosphorylation, which is caused by exposure to the saturated fatty acid, palmitate. In human liver cells, treatment with GW501516 has been shown to increase the adenosine monophosphate (AMP)/adenosine triphosphate (ATP) ratio and decrease the ATP/adenosine diphosphate (ADP) ratio, thus contributing to the prevention of insulin resistance[1].

In vivo Treatment with GW501516 alleviates NAFLD by modulating glucose and fatty acid metabolism[1].

Protocol

Animal Research:

[1]

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  • Animal Models: a model of non-alcoholic fatty liver disease (8-week-old male Sprague-Dawley rats)
  • Formulation: water
  • Dosages: 10 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (198.45 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 453.50
Formula

C21H18F3NO3S2

CAS No. 317318-70-0
Storage powder
in solvent
Synonyms Cardarine, GW1516

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID