Cardarine GW501516

Cardarine (GW501516) is a synthetic ligand of the Peroxisome Proliferator-Activated Receptor delta (PPAR-δ), originally developed by Ligand Pharmaceuticals and GlaxoSmithKline. It has been extensively studied in preclinical models for its metabolic regulatory properties, particularly in relation to lipid metabolism, endurance, and energy balance.

Research Focus Areas

• Activation of PPAR-δ Signaling Pathways:
  GW501516 exhibits high selectivity for PPAR-δ, with over 1000-fold specificity over other PPAR subtypes. Upon activation, it modulates transcription of genes related to fatty acid oxidation and energy utilization, notably increasing CPT1, CD36, and PGC-1α expression in skeletal muscle and liver tissues
• Metabolic Regulation in Animal or In Vitro Studies:
  Studies published by PNAS (https://www.pnas.org/doi/10.1073/pnas.0711875105) have demonstrated that GW501516 enhances fat metabolism, improves insulin sensitivity, and protects against diet-induced obesity and dyslipidemia
• Observed Effects on Endurance Markers in Controlled Environments:
  In a landmark study, Narkar et al. (2008)(https://pubmed.ncbi.nlm.nih.gov/18674809/) showed treatment with GW501516 significantly improved longer distances (+100 minutes endurance) compared to controls. The treatment promoted a “glucose-sparing” effect by increasing fat oxidation during physical activity.
• Energy Substrate Utilization in Laboratory Models:
  Metabolomic profiling indicated that Cardarine reprograms skeletal muscle fibers to favor oxidative metabolism, mimicking certain adaptations observed in trained endurance athletes

Potential Observations in Research

• Alterations in Lipid Profiles:
  In both rodent and primate studies, GW501516 has been shown to increase HDL (good cholesterol) and reduce triglyceride and LDL/VLDL levels
• Digestive Response Variations in Test Models:
  Some short-term studies report mild gastrointestinal irregularities, although these are model-dependent and not uniformly observed.

Handling and Dosage Information

Concentration range: 10–20mg/mL. Researchers may adjust the volume used based on the requirements of their protocol. In some settings, sublingual administration has been explored to assess absorption kinetics, but this is not a requirement for all study designs and remains a variable element depending on the delivery method used.

Important Notice:
This product is intended for laboratory research use only. It is not intended for human consumption, medical, veterinary, or household use. Keep out of reach of children.

FDA Disclaimer: The statements made within this website have not been evaluated by the US Food and Drug Administration. The statements and the products of this company are not intended to diagnose, treat, cure or prevent any disease. All products are for laboratory developmental research USE ONLY. Products are not for human consumption.

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