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LGD4033 (Ligandrol)

A Popular SARM undergoing clinical research.

$72.79

  • Active Ingredient: LGD4033
  • Strength: 10mg/ml
  • Each Bottle Contains: 30mg
 
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LGD-4033 (Ligandrol) is a selective androgen receptor modulator (SARM) that was developed by Ligand Pharmaceuticals and later licensed to Viking Therapeutics for clinical development. As a non-steroidal SARM, LGD-4033 binds to androgen receptors with high affinity and demonstrates strong tissue selectivity, producing potent anabolic effects in muscle and bone while exhibiting reduced activity in other androgen-responsive tissues.

LGD-4033 is among the most extensively studied SARMs in both preclinical and clinical settings. Its favorable oral bioavailability, potent anabolic effects, and tissue-selective profile make it particularly valuable for research into androgen receptor mechanisms and therapeutic applications for conditions involving muscle loss or bone fragility.

LGD-4033 Name and Classification

LGD-4033 is identified by multiple designations in scientific literature, including Ligandrol, VK5211 (Viking Therapeutics designation), and LGD. The compound belongs to the class of selective androgen receptor modulators and represents one of the most clinically advanced SARMs in development.

LGD-4033 was originally discovered by Ligand Pharmaceuticals as part of their SARM development program. The compound has progressed through multiple phases of clinical investigation for various conditions including age-related muscle loss, cancer-related cachexia, and hip fracture recovery.

Mechanism of Action

Like all SARMS, LGD-4033 functions by binding to androgen receptors with high affinity and selectivity, particularly in skeletal muscle and bone tissue. This selective activation triggers anabolic processes in target tissues while demonstrating reduced androgenic activity in others.

Key mechanistic features include:

  • Very high androgen receptor binding affinity among investigated SARMs
  • Tissue-selective activation with preferential activity in muscle and bone
  • Dose-dependent anabolic effects on muscle protein synthesis
  • Non-aromatizing properties - does not convert to estrogen
  • Oral bioavailability enabling convenient administration in research

In experimental models, LGD-4033 demonstrates potent ability to increase lean body mass, enhance muscle strength, and improve bone mineral density. The compound shows strong anabolic activity at relatively low doses compared to other SARMs and traditional androgens.

Benefits in Research

In preclinical and clinical research settings, LGD-4033 has been studied for its effects on muscle, bone, and overall body composition. Published studies suggest that LGD-4033 may:

  • Significantly increase lean body mass in a dose-dependent manner
  • Enhance muscle strength and physical function
  • Improve bone mineral density through androgen receptor activation
  • Preserve muscle mass in conditions of disuse or wasting
  • Demonstrate favorable anabolic-to-androgenic ratio in experimental models
  • Produce predictable dose-response relationships useful for research

These findings from controlled experimental models and human trials help researchers understand potent androgen receptor activation and the therapeutic potential of tissue-selective androgens for muscle and bone conditions.

LGD-4033 Dosage in Research Studies

Substantial data on LGD-4033 dosage comes from both animal research and human clinical trials. Published studies report varying protocols depending on research objectives and population studied.

Human clinical trial dosing:

  • 0.1 mg to 1.0 mg administered once daily in healthy volunteers
  • 1.0 mg daily commonly used in clinical efficacy studies
  • 0.3 mg and 1.0 mg daily evaluated in elderly populations
  • Dose-escalation studies to establish safety and efficacy thresholds

Animal model dosing:

  • 0.03-10 mg/kg in rodent studies depending on endpoints
  • Higher doses used to evaluate maximum effects and safety margins

Dosing considerations in research:

  • Oral administration is standard due to excellent bioavailability
  • Once-daily dosing is sufficient based on half-life of approximately 24-36 hours
  • Duration varies from short-term (weeks) to extended protocols (months)
  • Even low doses (0.1-1.0 mg in humans) produce measurable anabolic effects

The LGD-4033 dosage used in research directly impacts lean body mass gains, strength improvements, and degree of hormonal suppression. Clinical trials have demonstrated significant effects at doses as low as 1.0 mg daily, making LGD-4033 one of the most potent SARMs on a per-milligram basis.

LGD-4033 Side Effects in Research and Clinical Studies

Because LGD-4033 is a potent androgen receptor agonist, LGD-4033 side effects observed in research depend on dosage and duration. In human clinical trials and preclinical models, researchers monitor for:

Hormonal effects:

  • Dose-dependent testosterone suppression - significant at 1.0 mg daily in clinical trials
  • Suppression of LH and FSH through negative feedback on the HPG axis
  • Recovery of hormone levels following cessation, though time-dependent
  • No significant changes in estrogen levels due to non-aromatizing properties

Physical and metabolic observations:

  • Headaches reported in some clinical trial participants
  • Fatigue or lethargy in some subjects, potentially related to testosterone suppression
  • Mild increases in liver enzymes (ALT/AST) in some studies, generally reversible
  • Changes in lipid profiles including HDL reduction in some subjects
  • No significant cardiovascular safety concerns in clinical trials to date

Body composition effects:

  • Increased lean body mass - desired anabolic effect in muscle tissue
  • Decreased fat mass in some studies
  • Water retention reported by some subjects

Prostate and androgenic effects:

  • Minimal prostate-specific antigen (PSA) changes demonstrating tissue selectivity
  • Reduced androgenic effects on prostate compared to testosterone
  • No significant acne or hair loss reported in clinical trials

The LGD-4033 side effects profile in clinical trials has been generally favorable, with most adverse events being mild to moderate. The most significant concern is dose-dependent suppression of endogenous testosterone production, which appears reversible but may require extended recovery periods at higher doses or longer treatment durations. Understanding these side effects helps researchers establish appropriate dosing protocols and monitoring parameters for experimental use.

LGD-4033 and Hormonal Suppression

One important area of LGD-4033 research involves its effects on the hypothalamic-pituitary-gonadal axis. Clinical trials have demonstrated that LGD-4033 produces dose-dependent suppression of testosterone, with significant reductions observed at 1.0 mg daily over several weeks. Recovery of testosterone levels to baseline has been documented following cessation, though the timeframe varies based on dose and treatment duration. This suppression profile makes LGD-4033 valuable for studying SARM effects on endogenous hormone production and post-treatment recovery dynamics.

Oral Administration in Research

LGD-4033 demonstrates excellent oral bioavailability in both animal and human studies, making oral administration the standard route in research protocols. The compound's favorable half-life of approximately 24-36 hours allows for once-daily dosing, simplifying experimental protocols and improving compliance in clinical studies.

This allows researchers to examine sustained anabolic effects over extended treatment periods while investigating the pharmacokinetic characteristics of long-acting SARMs with predictable dosing schedules.

Human Clinical Trials

LGD-4033 has undergone multiple phases of human clinical trials, making it one of the most clinically studied SARMs. Phase I trials established safety and pharmacokinetics in healthy volunteers. Phase II trials evaluated efficacy in elderly populations for age-related muscle loss and in patients recovering from hip fracture.

Published clinical data demonstrates that LGD-4033 produces significant increases in lean body mass (approximately 1-2 kg over 3-12 weeks at 1.0 mg daily) with generally favorable tolerability. The compound has shown promise for therapeutic applications, though it has not yet received regulatory approval in major markets.

Why You Should Buy LGD-4033 from Sarmful

If you are looking to buy LGD-4033 for research purposes, we offers LGD-4033 for sale in liquid form, but also in powder form. Our LGD4033 is prepared to support consistent and reliable experimental work.

When you buy LGD-4033 from Sarmful, you benefit from:

  • Third-party lab testing and in-house verification for purity and concentration
  • EU and US domestic shipping for reliable delivery to your research facility
  • Convenient payment methods designed for seamless research procurement
  • Research-grade quality formulated to meet the standards of serious laboratory work

Clinical Trials in Healthy Adults

A Phase I clinical trial evaluated LGD-4033 safety, tolerability, and pharmacokinetics in healthy male volunteers. The study by Basaria et al. examined single ascending doses and demonstrated dose-proportional increases in plasma concentrations with a half-life of approximately 24-36 hours. Dose-dependent suppression of endogenous testosterone was observed, with recovery documented following cessation.

A landmark Phase II trial published in The Journals of Gerontology (2013) by Basaria et al. investigated LGD-4033 in healthy elderly men and postmenopausal women over 12 weeks. The randomized, double-blind, placebo-controlled study evaluated doses of 0.1 mg, 0.3 mg, and 1.0 mg daily. Results demonstrated significant dose-dependent increases in lean body mass, with the 1.0 mg group gaining approximately 1.21 kg of lean mass. Improvements in stair-climbing power and physical function were also observed with favorable tolerability.

Hormonal Effects and Body Composition

Multiple clinical trials have characterized LGD-4033's effects on the hypothalamic-pituitary-gonadal axis, demonstrating dose-dependent suppression of total testosterone (approximately 50-75% from baseline at 1.0 mg daily), luteinizing hormone, and follicle-stimulating hormone. Recovery studies show testosterone levels return toward baseline following cessation, though complete normalization may require several weeks to months. Body composition research consistently shows increases in lean mass with modest reductions in fat mass in some cohorts.

Preclinical Research

Preclinical studies in animal models demonstrated increases in bone mineral density in ovariectomized rats and enhanced muscle mass in various models of muscle wasting. Additional research has explored LGD-4033 in fracture healing and bone strength contexts. Comparative studies have established LGD-4033 as one of the most potent SARMs on a per-milligram basis.

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Research Data

Chemical Specification

PropertySpecification
Compound nameLGD-4033
Alternative namesLigandrol, VK5211
Chemical name4-[(2R)-2-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-2-(trifluoromethyl)benzonitrile
CAS number1165910-22-4
Molecular formulaC₁₄H₁₂F₆N₂O
Molecular weight338.25 g/mol
Chemical classSelective androgen receptor modulator (SARM)
Primary biological targetAndrogen receptor (AR)
Reported binding affinityAR Ki ≈ 1 nM (very high affinity)
Structure typeNon-steroidal benzonitrile derivative with trifluoromethyl and pyrrolidine groups
AppearanceWhite to off-white crystalline powder
ChiralityContains two chiral centers (R,R configuration)
Aqueous solubilityPoor / very low
Solubility – DMSOSoluble (commonly used stock solvent)
Solubility – EthanolSoluble
Solubility – PEG 400Soluble (frequently used for in vivo formulations)
Solubility – Propylene GlycolSoluble
Solubility – WaterPractically insoluble
StabilityStable as a dry solid under cool, dry, light-protected conditions
StorageStore at -20°C in tightly sealed container; protect from moisture and light
Half-lifeApproximately 24-36 hours (in human studies)
BioavailabilityExcellent oral bioavailability

Solubility Profile

SolventSolubility
WaterPractically insoluble
DMSOSoluble (~25+ mg/mL)
EthanolSoluble
PEG 400Soluble (commonly used for oral formulations)
Propylene GlycolSoluble
MethanolSoluble
DMFSoluble
AcetoneModerately soluble
ChloroformModerately soluble
HexaneInsoluble