LGD-4033 – Ligandrol

LGD-4033 – Ligandrol is one of the most researched, most requested non-steroidal SARMs in the Canadian research-chemical scene, and Helixx supplies it at high purity for lab work you can rely on. When a protocol needs a potent, orally active, high-affinity androgen-receptor ligand with a well-mapped human pharmacokinetic profile, Ligandrol is the reference-grade compound investigators keep reaching for.¹

What Is LGD-4033 – Ligandrol?

LGD-4033 (Ligandrol; developmental code VK5211; PubChem CID 44137686) is a non-steroidal, orally bioavailable selective androgen receptor modulator (SARM). Ligand Pharmaceuticals developed it, and Viking Therapeutics later carried it forward. Where anabolic-androgenic steroids are modified hormones, this is a small synthetic molecule built for tissue selectivity: it targets androgen receptors in skeletal muscle and bone while acting far more weakly on androgenic tissues such as the prostate. As one of the most studied Canadian SARMs, LGD-4033 – Ligandrol Canada is stocked by Helixx strictly as a reference material for in-vitro and pre-clinical investigation. It is not an approved drug, and WADA prohibits it in sport.

How LGD Works

LGD-4033 binds the ligand-binding domain of the androgen receptor (AR) tightly (reported Ki in the low-nanomolar range) and selectively. That binding drives a conformational change in the receptor, sends the AR-ligand complex into the nucleus, docks it onto androgen response elements (AREs) on DNA, and switches on tissue-selective transcription of the genes governing muscle protein synthesis and bone metabolism. Tissue selectivity is the whole point: in preclinical rodent models it behaves as a full or near-full agonist in muscle and bone while showing greater than 500-fold muscle-versus-prostate selectivity. In the published phase 1 human trial, 21 days of once-daily dosing produced dose-dependent, reversible gains in lean body mass with no significant change in fat mass. It also suppressed endogenous testosterone, SHBG, HDL cholesterol and triglycerides in a dose-dependent way, through feedback inhibition of the hypothalamic-pituitary-gonadal axis.¹

What the Research Shows

• Phase 1 human trial. A placebo-controlled study in 76 healthy young men (0.1, 0.3 and 1.0 mg/day for 21 days) found LGD-4033 was well tolerated, with no serious adverse events and no significant changes in liver enzymes, hematocrit, PSA or ECG, while producing dose-dependent gains in lean body mass.¹
• Linear, long pharmacokinetics. The same trial reported linear pharmacokinetics with a long elimination half-life (~24-36 h) and roughly threefold accumulation by day 21 of once-daily dosing. Suppressed hormones and lipids returned toward baseline after discontinuation.¹
• Hepatotoxicity at high off-label doses. A 32-year-old man taking approximately 10 mg/day (10-100x trial doses) developed severe drug-induced liver injury with jaundice, pruritus and bilirubin up to 35.0 mg/dL. Biopsy showed cholestatic hepatitis with mild fibrosis, which improved after cessation.²
• Cholestatic injury in the wider literature. Additional case reports describe severe cholestatic liver injury with bile-duct destruction after SARM use including ligandrol, generally recovering over roughly three months with supportive care.^{3 4}

Researchers who compare SARMs often benchmark Ligandrol against relatives such as RAD 140 – Testolone, MK2866 – Ostarine and YK11 – Myostine, and it frequently gets studied alongside the growth-hormone secretagogue MK-677 – Ibutamoren.

Chemical Properties

Research Protocols & Handling

All Helixx LGD-4033 – Ligandrol is supplied for laboratory, research and educational use only. It is not for human or veterinary consumption, and nothing here is dosing guidance. Handle it as a research chemical using appropriate PPE. Store the sealed compound cool, dry and out of direct light. Many investigators refrigerate the raw material for long-term stability, keep any reconstituted or solubilized working stock shielded from light, and use it within a short window. Confirm identity and purity against your own analytical standards before use, and dispose of research materials in accordance with your institution’s protocols.

Potential Side Effects & Safety

References

Peer-reviewed and authoritative sources cited above. Helixx supplies research materials for laboratory and educational use only; citations are provided for independent verification, not as medical guidance.

1. Basaria S, Collins L, Dillon EL, et al. The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men. J Gerontol A Biol Sci Med Sci. 2013;68(1):87-95. PMID: 22459616.
2. Barbara M, Dhingra S, Mindikoglu AL. Ligandrol (LGD-4033)-Induced Liver Injury. ACG Case Rep J. 2020;7(6):e00370. PMID: 32637435.
3. Koller T, Vrbova P, Meciarova I, et al. Liver injury associated with the use of selective androgen receptor modulators and post-cycle therapy: Two case reports and literature review. World J Clin Cases. 2021;9(16):4062-4071. PMID: 34141767.
4. Mohamed WT, Jahagirdar V, Fatima I, et al. Selective Androgen Receptor Modulators (SARMs)-Induced Liver Injury: A Case Report and Review of Literature. Cureus. 2023;15(2):e35094. PMID: 36945289.