Medchemexpress LLC Apalutamide | 956104-40-8 | 99.9% | 477.43 | 200 MG

Supplier:  Medchemexpress LLC HY16060200MG

Apalutamide is a potent and competitive antagonist of the androgen receptor (AR), binding to it with an IC50 of 16 nM. It is intended for research use.

• Exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor, potentially antagonizing GABAA at therapeutic dose levels.
• Targets the AR ligand-binding domain, preventing AR nuclear translocation, DNA binding, and transcription of AR gene targets.
• Shows low systemic clearance, high oral bioavailability, and a long plasma half-life in both mouse and dog, supporting once-daily oral dosing.
• Achieves increased steady-state plasma levels in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (2.5).
• Demonstrated significant tumor-volume reduction in castrate male mice bearing LNCaP/AR xenograft tumors.

Catalog No. 50-003-94404