GSK-2881078

GSK-2881078

GSK-2881078 is a potent, nonsteroidal selective androgen receptor modulator (SARM) originally developed by GlaxoSmithKline. Characterized as an orally bioavailable androgen receptor (AR) ligand, it serves as a critical tool compound in androgen receptor pharmacology research. It is frequently utilized in studies mapping AR signaling pathways and investigating the structure-activity relationships (SAR) inherent to the SARM compound class.

Technical Specifications

Mechanism of Action & Research Utility

GSK-2881078 functions by binding to the androgen receptor ligand-binding domain, effectively inducing AR-mediated transcriptional activation. Its potency is highlighted by an EC50 of approximately 3.99 nM in a PC3(AR)2 reporter cell assay, a response that can be successfully blocked using the AR antagonist bicalutamide.

Key research features include:

• High-Affinity AR Binding: The compound demonstrates high-affinity interaction with the androgen receptor.

• Tissue-Selective Profile: It exhibits differential transcriptional output between prostate-derived cell reporter assays and yeast androgen screens.

• Pharmacokinetic Utility: The compound has documented oral bioavailability in preclinical studies.

• Reference Standard: It is utilized as a reference ligand in mechanistic AR research and anti-doping analytical literature (including LC-MS method development).

Storage & Handling Guidelines

To maintain molecular integrity and ensure experimental reproducibility, adhere to the following protocols:

• Thermal Stability: Store the material at -20 °C for long-term stability.

• Environmental Conditions: Maintain in cool, dry conditions away from moisture.

• Light Protection: Ensure the compound is stored in light-protected conditions to prevent degradation.

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 formulation, clinical therapeutic, or diagnostic agent, and is strictly prohibited for human or veterinary consumption. Kimera Chems provides these high-purity chemical batches solely to accredited institutional laboratories and qualified scientific investigators.