ACP-105

ACP-105 is a non-steroidal androgen receptor (AR) agonist.¹ It increases proliferation in a receptor selection and amplification technology (R-SAT) assay using NIH3T3 cells expressing AR or AR containing a tyrosine-to-alanine substitution at position 877 (AR^T887A; EC₅₀s = 1 and 0.4 nM, respectively). ACP-105 (1 mg/kg per day) inhibits radiation-induced decreases in contextual fear conditioning freezing time, indicating a reversal of memory deficits, in female mice.² It reduces the frequency of time spent in the external and intermediate zone in an open field test, indicating anxiolytic-like activity, in combination with the non-steroidal estrogen receptor β (ERβ) agonist AC-186 (Item No. 33526) in a gonadectomized 3xTg mouse model of Alzheimer's disease when administered at a dose of 10 mg/kg per day for four months.³ ACP-105 (10 mg/kg per day for seven months), in combination with AC-186, decreases amyloid-β (1-40) (Aβ40) and Aβ42 levels in the brains, as well as increases the levels of ARs and the amyloid-β degrading enzymes neprilysin and insulin-degrading enzyme in the hippocampus, of gonadectomized 3xTg mice.

WARNING This product is not for human or veterinary use.

1. Schlienger, N., Lund, B.W., Pawlas, J., et al. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. J. Med. Chem. 52(22), 7186-7191 (2009).

2. Dayger, C., Villasana, L., Pfankuch, T., et al. Effects of the SARM ACP-105 on rotorod performance and cued fear conditioning in sham-irradiated and irradiated female mice. Brain Res. 1281, 134-140 (2011).

3. George, S., Petit, G.H., Gouras, G.K., et al. Nonsteroidal selective androgen receptor modulators and selective estrogen receptor β agonists moderate cognitive deficits and amyloid-β levels in a mouse model of Alzheimer’s disease. ACS Chem. Neurosci. 4(12), 1537-1548 (2013).