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3D molecular model of ACP-105

Calculated reference model · not an experimental or batch-certified structure. All 20 atoms shown.

Model data & sources
  • Heavy atoms only; hydrogens are omitted from the reference display.
  • Source-defined stereochemistry is checked against the calculated coordinates; no energy-minimum, crystal or solution-structure claim is made.
  • Reference molecular species only; batch identity, purity, counterions and excipients are not certified.
Formula
C16H19ClN2O
Method
RDKit ETKDGv3 / MMFF94s calculated reference conformer

ACP-105

By Kimera ChemsSelective Modulators

ACP-105 Research Standard

ACP-105 (CAS 899821-23-9) is a nonsteroidal benzonitrile (azabicyclooctane) selective androgen receptor modulator with partial agonist activity relative to testosterone, supplied as a reference standard for androgen receptor pharmacology. It came out of a high-throughput screen using receptor selection and amplification technology (R-SAT), and the same chemical series yielded potent antiandrogens alongside it — including one active at the AR T877A mutant.[1]

Mechanism of Action & Research Context

The molecular target is the androgen receptor (AR, NR3C4), a ligand-activated nuclear hormone receptor that functions as a transcription factor.

  • Partial agonism from a functional screen. ACP-105 was developed from an R-SAT high-throughput screen rather than from a binding assay, so it was selected on functional response from the outset.[1]

  • An agonist/antagonist series. The same scaffold produced both partial agonists and potent antiandrogens. One analogue antagonised the AR T877A mutant, a mutation of standing interest in receptor pharmacology because it changes ligand response. A series spanning both directions is more informative for SAR work than a set of agonists alone.[1]

  • Anabolic-parameter divergence. In a two-week study in castrated male rats, ACP-105 improved anabolic parameters.[1]

  • Distinct genomic and non-genomic routes. Nonsteroidal SARMs and endogenous androgens engage AR through different signalling arms and assemble different AR/cofactor complexes at androgen-responsive enhancers, so the two ligand types are not interchangeable in mechanistic work.[4]

  • Coregulator recruitment and dimerisation. A SARM can drive AR transcriptional activity while producing markedly less AR homodimerisation than DHT and recruiting only a restricted subset of cofactors, with p160 coactivators SRC1, TIF2 and NCoA3 notably absent in yeast two-hybrid assays. Differential coregulator recruitment is the leading mechanistic account of tissue selectivity.[5]

Research Applications

Primary fields of in vitro and preclinical laboratory investigation include:

  • Functional receptor screening including R-SAT and reporter-based transactivation assays.[1]

  • Structure-activity relationship work across a scaffold that yields both agonists and antagonists.[1]

  • Mutant-receptor pharmacology including AR T877A.[1]

  • In vitro metabolite identification — twelve phase I metabolites characterised in equine liver microsomes, the most of the seven SARMs in that study.[2]

  • Analytical and forensic method development. Reference material for chromatography-mass spectrometry identification, retention-time matching and metabolite characterisation.[3]

Analytical Documentation

Purity and identity vary by manufacturing lot. Kimera Chems does not publish a single fixed purity figure for this item; refer to the batch-specific Certificate of Analysis (COA) issued for the lot received, which reflects third-party analytical testing for that lot.

References

  1. Schlienger N, Lund BW, Pawlas J, et al. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. J Med Chem. 2009;52(22):7186–7191. doi:10.1021/jm901149c
  2. Cutler C, Viljanto M, Taylor P, Hincks P, Biddle S, Van Eenoo P. Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes. Drug Test Anal. 2022;14(2):349–370. doi:10.1002/dta.3189
  3. Stacchini C, Botrè F, Comunità F, et al. Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques. J Pharm Biomed Anal. 2021;195:113849. doi:10.1016/j.jpba.2020.113849
  4. Narayanan R, Coss CC, Yepuru M, et al. Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways. Mol Endocrinol. 2008;22(11):2448–2465. doi:10.1210/me.2008-0160
  5. Furuya K, Yamamoto N, Ohyabu Y, et al. Mechanism of the tissue-specific action of the selective androgen receptor modulator S-101479. Biol Pharm Bull. 2013;36(3):442–451. doi:10.1248/bpb.b12-00885

Storage & Handling

Store at controlled room temperature. Keep tightly closed. Liquid formats: do not refrigerate or freeze. Cold storage may cause the solution to cloud or precipitate. If this occurs, return to room temperature and mix until clear.

Storage guidance is a house recommendation. Analytical documentation is per-lot release testing.

Related Research Compounds

Research Use Only Disclaimer: This product is labeled and sold "For Research Use Only - NOT FOR HUMAN CONSUMPTION." It is not a drug, dietary supplement, food, cosmetic, or medical device, and it is not approved by the FDA or any other regulator for human or veterinary use. It is supplied to approved account holders as a research chemical for laboratory use and must be handled in accordance with applicable law.

Kimera Chems

Compounds That Survive Scrutiny

Research use only. Not for human or veterinary use.