ACP-105

ACP-105 is a non-steroidal androgen receptor (AR) agonist. 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 (ART887A, 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. 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 beta (ERbeta) agonist AC-186 (Cay-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. ACP-105 (10 mg/kg per day for seven months), in combination with AC-186, decreases amyloid-beta (1-40) (Abeta40) and Abeta42 levels in the brains, as well as increases the levels of ARs and the amyloid-beta degrading enzymes neprilysin and insulin-degrading enzyme in the hippocampus, of gonadectomized 3xTg mice.Formal Name: 2-chloro-4-[(3-endo)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]oct-8-yl]-3-methyl-benzonitrile. CAS Number: 899821-23-9. Molecular Formula: C16H19ClN2O. Formula Weight: 290.8. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Sparingly Soluble: 1-10 mg/ml. SMILES: ClC1=C(C=CC(N2[C@](C[C@](O)(C)C[C@@]32[H])(CC3)[H])=C1C)C#N. InChi Code: InChI=1S/C16H19ClN2O/c1-10-14(6-3-11(9-18)15(10)17)19-12-4-5-13(19)8-16(2,20)7-12/h3,6,12-13,20H,4-5,7-8H2,1-2H3/t12-,13+,16+. InChi Key: OUEODVPKPRQETQ-VIKVFOODSA-N.