ACP-105

ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC₅₀s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively. IC50 & Target: pEC50: 9.0 (AR wild type), 9.3 (AR T877A mutant)^[1]. In Vitro: ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC₅₀s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively. The half-lives of ACP-105 (compound 1) in human hepatocytes is measured and found to be 5.0 h^[1]. In Vivo: ACP-105 enhances freezing in both sham-irradiated and irradiated mice (effect of ACP-105: F=5.44; p=0.028). For MAP-2 immunoreactivity in the cortex of sham-irradiated mice, there is a brain area×ACP-105 interaction (F=6.655; p=0.0027). While ACP-105 reduces MAP-2 immunoreactivity in the sensorymotor cortex, there is a trend towards increased MAP-2 immunoreactivity in the enthorhinal cortex^[2].