What Is ACP-105?
ACP-105 is a nonsteroidal selective androgen receptor modulator (SARM) originally described in the medicinal chemistry literature (Bradley et al., J. Med. Chem. 2009) as part of a class of small-molecule androgen receptor ligands developed by Acadia Pharmaceuticals. In preclinical research models, ACP-105 has been characterized as a high-affinity partial agonist at the androgen receptor, with reported pEC₅₀ values of approximately 9.0 (AR wild-type) and 9.4 (AR T877A mutant).
Its receptor-binding profile and consistent in vitro signaling behavior have made ACP-105 a frequently referenced compound in androgen receptor pharmacology research and SARM structure-activity studies.
Chemical & Physical Properties
| Property | Description |
|---|---|
| Compound Class | Selective Androgen Receptor Modulator (SARM) |
| Chemical Type | Nonsteroidal small-molecule |
| IUPAC Name | 2-Chloro-4-[(1R,5R)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl]-3-methylbenzonitrile |
| CAS Number | 899821-23-9 |
| Molecular Formula | C₁₆H₁₉ClN₂O |
| Molecular Weight | 290.79 g/mol |
| Physical Form | Crystalline solid |
| Color | White to off-white |
| Solubility | Soluble in DMSO (~58 mg/mL); limited aqueous solubility |
| Stability | Stable under dry, light-protected conditions |
Mechanism of Action (Research Context)
ACP-105 binds to the androgen receptor ligand-binding domain and acts as a partial agonist, inducing receptor conformational changes associated with selective transcriptional activity in androgen-responsive cell models.
Reported mechanistic features include:
- High androgen receptor binding affinity (low-nanomolar range)
- Partial agonist activity at both wild-type and T877A mutant AR
- Differential transcriptional output across androgen-responsive cell types observed in preclinical models
- Orally bioavailable in published rodent pharmacokinetic studies
- Hepatic metabolism reported primarily via CYP3A4
These properties have supported ACP-105’s use as a reference ligand in mechanistic androgen receptor research.
Research Applications
ACP-105 is commonly referenced in experimental research involving:
- Androgen receptor binding and signaling pathway studies
- SARM structure-activity relationship (SAR) analysis
- Androgen-responsive gene expression and transcriptional assays
- Comparative SARM pharmacology research
- ADME and in vitro metabolism studies
- Analytical method development and reference-standard work
Handling & Storage Guidelines
- Store in a cool, dry location, protected from light
- Recommended storage: -20 °C for long-term stability
- Keep tightly sealed when not in use
- Use appropriate laboratory handling procedures and PPE
Important Research Disclaimer
ACP-105 is provided strictly for laboratory research use only (RUO). Not approved for human consumption, clinical use, veterinary use, or diagnostic purposes. No claims are made regarding safety, efficacy, or therapeutic application. All research involving this compound must comply with applicable laws and institutional guidelines.
| CAS Number | 1048998-11-3 |
| Other Names | ACP105, ACP 105, 899821-23-9, SCHEMBL4469384, CHEMBL3084681, AMY32474, ZKB82123, AKOS040741043, MS-24152, HY-112256, CS-0044397 |
| IUPAC Name | 2-chloro-4-[(1R,5S)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl]-3-methylbenzonitrile |
| Molecular Formula | C₁₆H₁₉ClN₂O |
| Molecular Weight | 290.79 |
