LGD-4033 (Ligandrol)

LGD-4033 (Ligandrol)

LGD-4033, also known as Ligandrol and by the developmental designation VK-5211, is a synthetic, nonsteroidal selective androgen receptor modulator (Selective Modulator). Originally developed by Ligand Pharmaceuticals and further advanced by Viking Therapeutics, it is one of the most extensively characterized compounds within the phenylpyrrolidine chemical class. In laboratory settings, it is utilized as a high-affinity reference ligand for investigating androgen receptor (AR) pharmacology, structure-activity relationships (SAR), and metabolic profiling.

Technical Specifications

Mechanism of Action & Research Utility

LGD-4033 acts as a tissue-differential AR ligand, binding to the androgen receptor ligand-binding domain with high affinity. Its binding induces a distinct receptor conformation compared to steroidal androgens, which results in selective transcriptional activity across different androgen-responsive cell types.

• Receptor Affinity: Reported binding $K_i approx 1 text{ nM}$.

• Functional Selectivity: Demonstrates full agonist activity in muscle- and bone-derived cell models, with reduced (partial agonist) activity observed in prostate-derived reporter models.

• Metabolic Profile: Well-characterized metabolite profile used in forensic and analytical toxicology research.

Research Applications

LGD-4033 is a foundational reference compound for studying androgen signaling and analytical method development.

Primary fields of in vitro and ex vivo laboratory investigation include:

• Receptor Pharmacology: Androgen receptor binding, competition, and transactivation assays.

• SAR Analysis: Investigating structure-activity relationships within the phenylpyrrolidine structural class.

• Selectivity Profiling: Nuclear receptor selectivity assays against the broader steroid hormone receptor family.

• Conformation Studies: AR ligand-binding domain conformation and coregulator recruitment dynamics.

• Analytical/Forensic Work: Extensive use in developing LC-MS/MS methods for detection and metabolic/ADME research.

• Comparative Research: Evaluating AR ligand behavior alongside other Selective Modulators such as LGD-3303 and LGD-2226.

Storage & Handling Guidelines

To maintain the structural integrity and stability of the research material:

• Long-Term Storage: Store powder at -20 °C.

• Short-Term Storage: Room temperature is acceptable for active research use.

• Environmental Control: Protect from direct light and keep in a tightly sealed container to prevent degradation.

• Moisture Protection: Use desiccant for powder storage.

• Handling: Adhere to appropriate laboratory handling procedures and wear required Personal Protective Equipment (PPE).

Regulatory & Research Use Disclaimer

Research Use Only Disclaimer: This product is developed and distributed strictly as a Research Use Only (RUO) laboratory reference chemical intended exclusively for non-clinical analytical and scientific investigation. It is not intended for human consumption, clinical use, veterinary use, therapeutic application, dietary supplement use, or diagnostic purposes. LGD-4033 is included on the World Anti-Doping Agency (WADA) Prohibited List under the anabolic agents category, and the FDA has issued advisories regarding its misuse. All handling, preparation, and experimental use must comply with applicable federal, state, and local laws, as well as institutional laboratory safety standards. Kimera Chems supplies this reagent exclusively to qualified researchers and scientific institutions.