Cardarine

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

Related by research scope · open each to compare

GW-501516 is not an approved drug and has no authorized human use in the United States. It is not scheduled as a controlled substance under the DEA Controlled Substances Act but may not be sold for human consumption. Because it is a small molecule — not a peptide — it is not part of the 2025–2026 FDA Category 2 bulk drug substances review (docket FDA-2025-N-6895) affecting compounded peptides.

Confirmed high-severity market-integrity event (enforcement / recall / counterfeit)

Transparent blend · bci-1.0 · never paid-placement

Primary name

Cardarine

Origin

GW-501516 was synthesized during a collaborative program between Ligand Pharmaceuticals and GlaxoSmithKline in the early 1990s, originally intended to treat dyslipidemia, metabolic syndrome, and cardiovascular disease. Despite early favorable Phase I/II signals in human lipid biomarker studies, the full development program was abandoned around 2006–2007 when long-term rodent carcinogenicity studies revealed rapid multi-organ tumor formation. It has no approved indication in any jurisdiction. CAS 317318-70-0; PubChem CID 9803963; DrugBank DB05416.

Registry IDs

PubChem CID

9803963

CAS

317318-70-0

InChIKey

YDBLKRPLXZNVNB-UHFFFAOYSA-N

DrugBank

DB05416

ChEMBL

CHEMBL38943

Molecular formula

C21H18F3NO3S2

Molar mass

453.5 g/mol

Monoisotopic

453.06802027 Da

InChIKey

YDBLKRPLXZNVNB-UHFFFAOYSA-N

Appearance

White to off-white crystalline powder

Solubility

Poorly soluble in water; soluble in DMSO and other polar organic solvents. DMSO …

Sequence not available in current seed.

Stability: Stable as dry solid under recommended cold-chain conditions. Hydrolytic stability in aqueous solution is limited; solutions in DMSO are more stable. Formal peer

Vial sizes

null mg

Purity grades

≥98% (HPLC) / ≥99% (HPLC)

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• GW-501516 binds selectively to PPARδ (also termed PPARβ/δ) with high affinity (EC50 approximately 1.1–1.2 nM), acting as a full agonist of this nuclear receptor transcription factor
• Upon receptor binding, the PPARδ/RXR heterodimer activates peroxisome proliferator response elements (PPREs) in gene promoter regions, upregulating transcription of proteins involved in fatty acid transport (FABP3), mitochondrial fatty acid oxidation (CPT1, PDK4), and mitochondrial biogenesis
• In preclinical muscle and adipose tissue models, this produces a metabolic shift toward lipid substrate utilization, reduced triglyceride accumulation, elevated HDL cholesterol, and enhanced oxidative capacity
• The same transcriptional program that governs metabolic adaptation is also implicated in cell-cycle dysregulation: PPARδ activation promotes expression of growth-promoting genes, which in chronic-exposure rodent studies was associated with accelerated tumor development across multiple organs

Pharmacokinetics (ADME)

Half-life

Not formally characterized in published peer-reviewed literature; no validated human PK data available following development abandonment

Clearance

null

PK–PD note: GSK conducted early Phase I studies examining lipid biomarker effects, but PK parameters were not disclosed in the public domain following program cancellation. A hair-matrix detection method was publ…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Oliver et al. 2001, PNAS 98:5306 — discovery: 'A selective PPARδ agonist promotes reverse cholesterol transport' — The seminal paper introducing GW501516; in vitro + insulin-resistant obese rhesus-monkey data.
• Sprecher et al. 2007, ATVB 27(2):359-365 — first PPARδ agonist dosed in humans (PMID 17110604) — n=24 healthy volunteers; randomized, placebo-controlled 2-week first-in-man study. No NCT (predates registry mandates).
• Ooi et al. 2011, J Clin Endocrinol Metab 96(10):E1568-76 (NCT00841217) — n=13 dyslipidemic men; randomized, placebo-controlled crossover; lipoprotein kinetics (apoB/apoC-III/apoA-II).
• Olson et al. 2012, ATVB 32(9):2289-2294 (NCT00158899, GSK protocol PAD20001) — The largest completed human GW501516 RCT; n=268 analyzed (424 enrolled); dose-dependent lipid effects vs placebo and fenofibrate.
• Narkar et al. 2008, Cell 134(3):405-415 — 'AMPK and PPARδ Agonists Are Exercise Mimetics' — Landmark rodent mechanism paper (GW501516 + training reprogram muscle fiber type/endurance). Mouse study, not a human trial.
• Mitchell & Bishop-Bailey 2019, Pulmonary Circulation — PPARβ/δ 'blighted by cancer risk' — Closest anchoring narrative synthesis of the trial history + unresolved cancer debate; notes the 104-week rat/mouse carcinogenicity data exist only as 2009 SOT conference abstracts, never full peer-reviewed papers.

No registered human trials found for this compound.

Status

No registered trials found

Summary (literature)

The pivotal safety finding for GW-501516 is rapid multi-organ carcinogenesis in long-term rodent studies. In rats and mice administered doses of 3–30 mg/kg/day for up to 104 weeks, tumor formation was observed across liver, stomach, urinary bladder, colon, skin, and tongue, with …

WADA status

Prohibited at all times under the WADA 2026 Prohibited List, classified under S4.4 (Metabolic Modulators — PPARδ agonists). GW-501516 has been on the WADA Prohi…

Dominant research route: Oral. Every registered human clinical trial (the GSK Phase I–II program, plus the later academic Phase-II/IV metabolic-syndrome and cardiac-energetics studies) dosed GW501516 by mouth, and the core preclinical exercise-endurance/metabolic literature (e.g. Narkar et al. 2008) also dosed rodents orally. Intraperitoneal injection appears only in isolated mechanistic/oncology xenograft rodent work outside that core program; no intramuscular, intravenous, or subcutaneous human or animal study was identified.

The only route formally tested in registered human trials: at least four ClinicalTrials.gov records (NCT00158899, NCT00318617, NCT00388180, NCT00841217) from the 2000s GSK/academic program, plus the separate randomized, placebo-controlled first-in-man study in 24 healthy volunteers dosed 2.5 mg or 10 mg once-daily for 2 weeks (Sprecher et al. 2007, ATVB). Also the dosing route in the pivotal rodent efficacy work and the unpublished 104-week rat/mouse carcinogenicity bioassays that led to program discontinuation.

Bioavailability: No published absolute oral-bioavailability percentage identified for any species. Oral dosing produced measurable, quantified pharmacodynamic effects in humans (HDL-C up, triglycerides/LDL-C trending down at 2.5–10 mg/day) and rodents (PPARδ target-gene induction, running-endurance gains at ~5 mg/kg/day); urinary metabolites detectable for weeks after a single oral dose — absorption itself is not the open question here.

The route in every registered human trial and the core rodent literature; also the format the research-chemical market predominantly sells (oral liquid, capsule, tablet). No human dosing recommendation is implied — the trials describe a discontinued, never-approved investigational program, not a protocol for use.

Used as a systemic dosing route in isolated mechanistic/oncology mouse xenograft work (e.g. nasopharyngeal-carcinoma tumorigenicity in BALB/c nude mice, 10 or 30 mg/kg once daily × 4 weeks), not in the core metabolic/exercise program, which dosed orally. Animal-only; not a human route.

Bioavailability: No dedicated IP pharmacokinetic characterization identified; IP was used as a laboratory dosing route to test tumor biology, not to study absorption or kinetics.

A laboratory-animal administration route cited only to describe how a subset of mechanistic/oncology work was conducted; no human-use pathway.

No published pharmacological or skin-absorption study identified for GW501516 by this route. Multiple online research-chemical vendors market a topical gel/transdermal-solution format, but this is a commerce offering, not literature-backed research.

Bioavailability: No transdermal absorption, bioavailability, or pharmacokinetic data exist for GW501516 in any species.

Vendor-marketed format only; no study establishes whether clinically meaningful systemic exposure is achieved via skin application. No human use or benefit implied.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Weekly median $/mg from the live vendor crawl.

Researched storefront prices, bucketed

p25 $0.100 · median $0.120 · p75 $0.170 · 12 researched vendors

Legit, COA-backed band: $0.100–$0.200/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$1

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Purity on the current market (researched)

US/CA vendor product pages for Cardarine/GW-501516 near-universally advertise ~98–99%+ HPLC purity with a linked COA (e.g. Sports Technology Labs cites 99.57% via MZ Biolabs; Behemoth Labz and Element SARMs each claim ~99%). These are vendor-published/self-reported results, not an independent cross-vendor aggregate — no Finnrick-style multi-hundred-sample GW-501516 purity survey was found. The best available independent QC data point is market-adjacent, not Cardarine-specific: Van Wagoner et al. 2017 (JAMA) chemically analyzed 44 internet-sold products marketed as SARMs — only 41% (18/44) matched the labeled active-compound amount, 9% (4/44) contained no active compound, and 39% (17/44) contained a DIFFERENT unapproved drug than labeled, with GW501516 named as one example among them (alongside ibutamoren/MK-677 and SR9009). [Verification corrected an over-specific first-pass phrasing that read the 39% as a GW501516-specific rate — it is a category proportion.]

Independent labs cited for this compound

No FDA-issued Class I/II/III recall of a Cardarine/GW-501516 product was found (verified against openFDA drug + food enforcement, current to 2026-07-01). As an unapproved new drug sold outside the regulated supply chain, US enforcement takes the form of warning letters, criminal referral/guilty pleas and import detention rather than recalls (the only SARM-class drug recall on record, D-0800-2020 Class II, is for a different compound, RAD-140). Health Canada did take a genuine recall-like action — advisory RA-73367 named and seized specific Cardarine products (see events[]) — reported honestly rather than omitted.

Buyer red-flag checklist

• Marketed/sold under the 'SARM' umbrella despite GW-501516 actually being a PPARδ agonist with an unrelated mechanism — a labeling/category confusion common across vendor sites (and echoed in several FDA letters).
• No batch-specific COA provided on request (community convention: assume underdosed or contaminated).
• COA/report ID does not resolve in the testing lab's own public verification database (Janoshik, MZ Biolabs, Colmaric).
• Purity-only COA with no LC-MS/GC-MS identity confirmation — cannot rule out a different compound; documented precedent of 'SARM'-labeled products actually containing testosterone (DOJ, Kawa/Stechkober/Paradigm case, guilty plea Dec 2025) and of GW501516 appearing as an undeclared ingredient in other labeled SARM products (Van Wagoner 2017 JAMA).
• Vendor copy marketed for 'fat loss'/'endurance'/human-use benefit rather than as research material — the labeling pattern that has repeatedly drawn FDA warning letters (Umbrella 2021; SARMS AMERICA + the Dec 2025 multi-vendor sweep).
• 'Research use only' disclaimer paired with explicit human dosing/cycle instructions on the same page.
• Price far below the prevailing vendor-market norm for the claimed mg/mL concentration (consistent with an underfilled or off-spec product).

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No independent lab aggregate (Janoshik/MZ Biolabs/Finnrick-style) specific to products labeled/sold as Cardarine/GW-501516 was found, so no prevalence figure is reported — an honest null, not an invented one. The closest data is market-adjacent: Van Wagoner et al. 2017 (JAMA, n=44 products marketed as SARMs) found 18/44 (41%) matched their labeled active-compound amount, 4/44 (9%) contained no active compound, and 17/44 (39%) contained a different unapproved drug than labeled (GW501516 one named example among them). Documents systemic QC risk in the same grey channel that sells Cardarine, but is not a Cardarine-labeled-product-specific dosing-accuracy statistic. [A vendor-guide claim that '75% of online SARMs' / 'most GW-501516' is fake was refuted as an uncited marketing estimate and is NOT carried as a data point.]

• FDA Import Alert 66-41 ('Detention Without Physical Examination of Unapproved New Drugs Promoted In The U.S.', most recently republished 2026) is the DWPE mechanism FDA applies to unapproved-new-drug research chemicals sold online — the posture used for SARM/PPARδ-agonist products like Cardarine/GW-501516 marketed 'research use only'. It is not GW-501516-specific — no dedicated Cardarine/SARM import alert was found — and DWPE hits firms/products placed on the alert's Red List, not the molecule categorically. An RUO label is not an import exemption; CBP/FDA judge actual intended use.66-41 (unapproved new drugs promoted in the U.S.)
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Prohibited at all times (in- and out-of-competition) on the WADA Prohibited List under S4 — Hormone and Metabolic Modulators, specifically S4.4.1 (PPARδ agonists) on the current 2025/2026 List; a non-specified substance (confirmed by the AIU and the primary WADA List). No FDA-approved human therapeutic use exists, so there is no Therapeutic Use Exemption pathway. Multiple athletes (Issam Asinga, Adaejah Hodge) and a coach (Gerald Phiri) were sanctioned 2024–2025 for GW1516/Cardarine positives or possession. (USADA's page still shows the retired 'S4.5' number and characterizes the compound as having 'not undergone human studies' — attributed to USADA; note 3 completed biomarker RCTs are on record, see evidence.)

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• Vendor-affiliated SEO/review blogs and product pages dominate 'where to buy' and purity-claim content, with a commercial incentive to reassure buyers (a widely-circulated '75% of online SARMs are fake / most GW-501516 is 100% fake' figure comes from such a vendor guide and is refuted — excluded, see quality)
• Survivorship / enthusiasm bias — dramatic before/after endurance and fat-loss anecdotes over-shared vs null-result reports
• Doping-ban news cycles (collegiate and Olympic-level cases) skew framing toward detection/risk rather than typical recreational-use experience
• Placebo / concurrent-stack confounding — Cardarine is rarely reported alone; concurrent SARMs, diet and training changes co-occur in most anecdotes
• Athlete self-defense narratives ('contaminated supplement') may understate deliberate use and complicate an honest tone read
• Negativity bias in cancer-risk and counterfeit-warning threads relative to the larger volume of neutral-to-positive cardio/fat-loss discussion

Manually researched from reddit, youtube, x— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

Abandoned PPARδ agonist (GW-501516) studied in rodents for metabolic and endurance effects; development halted due to multi-organ carcinogenicity. Approximately 9 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Not FDA-approved; research use only; not subject to FDA-19 peptide compounding framework. Research use only.

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