ACP-105是一种可口服的、有选择性的、有效的雄激素受体调节剂(SARM),其对野生型AR和T877A突变型AR的pEC50值分别为9.0和9.3。
CAS：899821-23-9
分子式：C16H19ClN2O
分子量：290.79
纯度：98%
存储：Store at -20°C

Background:

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.

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].

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].

[1]. Schlienger N, et al. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. J Med Chem. 2009 Nov 26;52(22):7186-91. [2]. Dayger C, et al. Effects of the SARM ACP-105 on rotorod performance and cued fear conditioning in sham-irradiated and irradiated female mice. Brain Res. 2011 Mar 24;1381:134-40.