RAD-140 (Testolone)

RAD-140 (Vosilasarm / Testolone) Research Standard

RAD-140, also known as Vosilasarm (Testolone), is a synthetic nonsteroidal selective androgen receptor modulator (SARM) with high-affinity binding characteristics for the androgen receptor (AR). Originally developed for its tissue-specific anabolic properties, it has advanced into clinical investigation, particularly for the treatment of AR-positive hormone-sensitive breast cancer. In laboratory settings, RAD-140 serves as a high-precision reference standard for studying nuclear receptor signaling, structure-activity relationships (SAR) within the benzonitrile-oxadiazole class, and the development of analytical methods for detecting Selective Modulators in complex matrices.

Technical Specifications

Mechanism of Action & Research Context

RAD-140 functions as a tissue-differential ligand, meaning it elicits distinct transcriptional outcomes depending on the receptor environment and coregulator recruitment.

• Receptor Binding: RAD-140 exhibits high affinity for the androgen receptor ligand-binding domain. Its interaction promotes a unique conformational shift distinct from endogenous steroidal androgens, which is a primary focus of structural biology studies.

• Transcriptional Output: Research demonstrates full-agonist activity in muscle- and bone-derived cell models, while exhibiting partial-agonist or suppressive activity in other tissue types.

• Oncology Research: In AR+/ER+ breast cancer research, the compound is studied for its dual role: acting as an AR agonist while simultaneously suppressing ER-mediated signaling and downregulating ESR1 mRNA expression.

• Metabolic Profile: Preclinical data identifies hepatic metabolism via oxidation and conjugation pathways, providing a framework for ADME (Absorption, Distribution, Metabolism, and Excretion) studies in isolated liver models.

Research Applications

RAD-140 is a widely recognized reference standard for advanced pharmacological and analytical research.

Primary fields of in vitro laboratory investigation include:

• Androgen Receptor Signaling: Utilizing competitive binding and transactivation assays to map AR-ligand interaction dynamics.

• Oncology & Nuclear Receptor Crosstalk: Investigating the interaction between AR and ER pathways in hormone-sensitive breast cancer models.

• Analytical Method Development: Serving as a primary reference standard for LC-MS/MS protocols in anti-doping forensic toxicology.

• SAR Analysis: Evaluating how the oxadiazole heterocycle and nitrile substituents contribute to receptor selectivity and metabolic stability.

• Toxicological Assessment: Analyzing hepatotoxicity potential and cellular stress markers in response to prolonged ligand exposure.

Storage & Handling Guidelines

To maintain the chemical stability and experimental reliability of the compound:

• Long-Term Storage: Store in a dry, cool environment. For maximum stability, maintain at -20 °C.

• Atmospheric Control: Keep the container tightly sealed to prevent degradation.

• Light Sensitivity: Protect from direct light to preserve the integrity of the benzonitrile-oxadiazole scaffold.

• Aseptic Technique: Utilize clean, non-reactive laboratory equipment to prevent contamination, particularly when preparing stock solutions for binding assays.

Regulatory & Research Note

RAD-140 is designated as a prohibited substance on the World Anti-Doping Agency (WADA) list. Researchers involved in anti-doping analytical chemistry use this compound as a certified reference material for developing detection methods for non-medical use. The compound is under active clinical study (e.g., EP0062) for oncological indications; it is not approved for any consumer, medical, or dietary application.

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 an FDA-approved drug, medical treatment, dietary supplement, or food ingredient, and is strictly prohibited for human or animal consumption. Kimera Chems supplies this high-purity research material solely to qualified institutions and professional investigators for authorized laboratory research.