SARMs

Cardarine (GW-501516)

Evidence: animal_plus_anecdotal

Mechanism of Action

Cardarine is a selective peroxisome proliferator-activated receptor delta (PPARd) agonist, not a SARM (it does not bind the androgen receptor). PPARd activation in skeletal muscle upregulates genes for fatty acid oxidation (CPT1B, PDK4, ACOX1), shifting fuel substrate from glycolysis toward beta-oxidation, effectively increasing endurance capacity and fat utilization. It increases oxidative type I (slow-twitch) muscle fiber proportion, enhances mitochondrial biogenesis via PGC-1a coactivation, reduces circulating triglycerides and LDL, and increases HDL cholesterol. PPARd activation also reduces macrophage-mediated inflammation through NF-kB suppression.

Dosing Protocol

Standard: Research indicates 10-20 mg daily orally for 8-12 weeks. Clinical trials (metabolic syndrome) used 2.5-10 mg/day.

Maintenance: Research indicates 10 mg daily. Some users report efficacy at 10 mg with diminishing returns above 20 mg.

Administration: oral

Timing: Once daily, 1-2 hours before exercise for acute endurance benefit. Half-life approximately 16-24 hours. Consistent daily dosing.

Duration: 8-12 week cycles. No HPG suppression, so PCT is not required. However, long-term safety is unknown and cycling is prudent.

Notes

CRITICAL SAFETY WARNING: GW-501516 development was abandoned by GlaxoSmithKline in 2007 after 2-year carcinogenicity studies in rats showed accelerated tumor development in multiple organs (liver, bladder, stomach, skin, thyroid, tongue, testes, ovaries, uterus) at ALL doses tested, including doses close to the human therapeutic range. The cancer risk is the dominant consideration for this compound. Proponents argue that 2-year continuous dosing in rats doesn't translate to intermittent human use, but this is unproven. Cardarine does not suppress the HPG axis or testosterone — it is not a SARM by mechanism. It does not require PCT. Required bloodwork: Liver function panel, lipid panel, fasting glucose, CBC at baseline and every 4-6 weeks. Cancer screening appropriate for age and risk factors. This compound carries a uniquely concerning safety profile. Medical supervision required.

Stacking

  • Ostarine (popular body recomposition stack — cardarine adds fat loss/endurance without hormonal suppression)
  • SR-9009 (complementary metabolic mechanisms)
  • MK-677 (recovery and appetite counter to cardarine's potential appetite reduction)

Interactions

  • Diabetes medications (metformin, sulfonylureas) [MEDIUM] — Additive glucose-lowering and lipid-modifying effects. Monitor for hypoglycemia.
  • Statins [LOW] — Additive lipid improvement — may allow statin dose reduction under medical supervision.
  • Anticoagulants [LOW] — PPARd agonism may affect platelet function; theoretical interaction.

Contraindications

  • Active or history of cancer (CRITICAL — see notes on carcinogenicity)
  • Pregnancy and breastfeeding
  • Individuals under 21
  • Liver disease

Side Effects

  • CANCER RISK: Accelerated tumor development in multiple organs observed in 2-year rodent study at all doses tested
  • Headache
  • Nausea
  • Diarrhea
  • Potential liver effects at high doses

Key Papers

  • 10.1073/pnas.0306033100
  • 10.1016/j.cmet.2008.06.006
  • 10.1371/journal.pone.0115346

Source Quality

Not FDA-approved. Clinical development abandoned in 2007 due to carcinogenicity findings. Research chemical only. WADA-prohibited substance since 2009. Source with extreme caution — analytical verification essential.

Disclaimer: This information is for educational purposes only and is not medical advice. BioAccelera Labs does not diagnose, treat, or prescribe. Consult a licensed healthcare provider before using any compound.

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