Informational only. Not medical advice.INFORMATIONAL PLATFORM ONLY — NOT MEDICAL ADVICE, DIAGNOSIS, OR TREATMENT
Informational only. Not medical advice.INFORMATIONAL PLATFORM ONLY — NOT MEDICAL ADVICE, DIAGNOSIS, OR TREATMENT
Head-to-head comparison of Amlexanox and Cardarine (GW-501516) — mechanism, side effects, legal status, and pricing.
Amlexanox is a non-peptide small-molecule 2-amino-chromeno[2,3-b]pyridine-3-carboxylic acid derivative (CAS 68302-57-8, MW 298.29 g/mol). Originally approved in 1996 as a topical oral paste for aphthous ulcers (FDA, now discontinued) and in Japan for allergic conditions, it was later characterized as a selective ATP-competitive inhibitor of the non-canonical IκB kinases TBK1 and IKKε. It is NOT approved for any metabolic, obesity, or performance indication; it is sold by research-chemical vendors labeled research-use-only and promoted off-label by biohacking outlets for fat loss. No validated human dose exists for metabolic applications.
Cardarine (GW-501516) is a synthetic small-molecule PPARδ agonist — not a SARM and not a peptide, despite gray-market marketing that groups it with SARMs. Developed by GSK and taken into human lipid trials, its clinical development was discontinued around 2007 after rodent carcinogenicity findings. It has no regulatory approval anywhere, is WADA-prohibited at all times, and is sold only as a gray-market research chemical.
Amlexanox
Cardarine (GW-501516)
Category
Legal Status
Mechanism
Side Effects
COA-verified vendors · trust score ≥70 required · single-vial price — bulk/bundle deals may be lower
Amlexanox
Cardarine (GW-501516)
COA corpus from Disclosed Labs — independently tested batches only.
Amlexanox
1
COAs
99.6%
Avg purity
1
Labs
Cardarine (GW-501516)
2
COAs
99.7%
Avg purity
1
Labs
In diet-induced obese and ob/ob mice, amlexanox treatment increased energy expenditure via thermogenesis, produced weight loss, improved insulin sensitivity, and decreased hepatic steatosis; these metabolic benefits require intact FGF21 signaling. In LDL-receptor-knockout mice on Western diet, amlexanox reduced triglycerides, cholesterol, circulating monocytes/eosinophils, macrophage plaque accumulation, and atherosclerotic lesion size. One randomized, double-blind, placebo-controlled proof-of-concept trial in 42 obese patients with type 2 diabetes and NAFLD showed statistically significant HbA1c and fructosamine reductions versus placebo, with a responder subgroup showing improved insulin sensitivity and reduced hepatic fat; rash occurred in several participants (two required biopsy). No obesity or diabetes indication has been approved by any regulator.
Completed GSK-sponsored human trials in low-HDL/dyslipidemia subjects (2.5–10 mg/day, 12 weeks) improved lipids (HDL-C +16.9%, triglycerides −16.9%, LDL −7.3%; Sprecher et al., 2012). GSK halted development around 2007 after a 2-year rodent carcinogenicity study reported tumors across multiple organs; a 2019 mouse study found GW-501516 accelerated colitis-associated colorectal cancer. A published human case report documented severe rhabdomyolysis and hepatotoxicity from self-administration. Never approved for any indication; not a peptide.
Amlexanox and Cardarine (GW-501516) are both in the Metabolic category and may have overlapping mechanisms. Researchers should review both profiles carefully, understand the mechanisms of action, and monitor the relevant biomarkers when combining compounds in the same class. As always, consult a licensed healthcare provider before making any decisions about combining research compounds.
This platform provides informational tools only, not medical advice. This comparison is for educational purposes only. Consult a licensed provider.
Contraindications
Lab Testing
Disclosed Labs