RU58841 (PSK-3841) Research Standard

RU58841 (PSK-3841/HMR-3841) is a potent, non-steroidal antiandrogen utilized extensively in molecular biology research as a high-affinity competitive antagonist of the androgen receptor (AR). Characterized by its benzonitrile core, trifluoromethyl group, and imidazolidinedione ring, this compound is engineered to occupy the receptor pocket with high selectivity. In laboratory settings, RU58841 serves as a critical reference ligand for mapping receptor-ligand docking interactions and conducting competitive binding assays to delineate the pharmacodynamics of AR-mediated signaling.

Technical Specifications

Mechanism of Action & Research Context

RU58841 functions as a competitive inhibitor at the androgen receptor, preventing the binding of endogenous androgens and subsequent receptor activation.

• Receptor Binding Pocket: The molecule’s trifluoromethyl and imidazolidinedione moieties are strategically designed to facilitate high-affinity binding within the AR ligand-binding domain (LBD). Researchers utilize this to explore the steric and electronic requirements of the binding pocket.

• Competitive Inhibition: In cell-free and in vitro models, RU58841 is used to effectively block native androgenic ligands. This allows investigators to generate dose-response curves and calculate the inhibition constants (K_i) necessary for detailed pharmacological mapping.

• Structural Biology: The compound serves as a probe to identify specific contact points between ligands and the AR, aiding in the structural characterization of the receptor’s activation-inhibition dynamics.

Research Applications

RU58841 is a specialized reagent essential for biochemical assays and receptor research.

Primary fields of in vitro laboratory investigation include:

• Competitive Binding Assays: Measuring the binding strength of RU58841 against various androgen receptor preparations to evaluate affinity.

• Receptor-Ligand Docking Mapping: Using the compound to identify the physical orientation and binding footprint within the androgen receptor.

• Structure-Activity Relationship (SAR) Studies: Investigating how the benzonitrile core and trifluoromethyl group modulate binding potency.

• Vehicle/Carrier Compatibility: Utilizing the provided ethanol/DMI/propanediol system to study the influence of carrier vehicles on topical delivery and penetrative efficacy in experimental tissue models.

Storage & Handling Guidelines

Store at controlled room temperature. Keep tightly closed. Liquid formats: do not refrigerate or freeze. Cold storage may cause the solution to cloud or precipitate. If this occurs, return to room temperature and mix until clear.

Storage guidance is a house recommendation. Analytical documentation is per-lot release testing.