Chemistry:AC-262,536

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Short description: Chemical compound
AC-262,536
AC-262,356.svg
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC18H18N2O
Molar mass278.355 g·mol−1
3D model (JSmol)
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AC-262536 is a drug developed by Acadia Pharmaceuticals which acts as a selective androgen receptor modulator (SARM). Chemically it possesses endo-exo isomerism, with the endo form being the active form. It acts as a partial agonist for the androgen receptor with a Ki of 5 nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of the levator ani muscle weight increase of testosterone, but only around 27% of its maximal effect on prostate gland weight.[1][2][3] It is an aniline SARM related to ACP-105 and vosilasarm (RAD140).[4]

References

  1. "Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator". J Steroid Biochem Mol Biol 109 (1–2): 129–37. March 2008. doi:10.1016/j.jsbmb.2007.11.001. PMID 18164613. 
  2. "Equine metabolism of the selective androgen receptor modulator AC-262536 in vitro and in urine, plasma and hair following oral administration". Drug Testing and Analysis 13 (2): 369–385. February 2021. doi:10.1002/dta.2932. PMID 32959959. https://biblio.ugent.be/publication/8694577. 
  3. "Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques". Journal of Pharmaceutical and Biomedical Analysis 195: 113849. February 2021. doi:10.1016/j.jpba.2020.113849. PMID 33383501. 
  4. "Deciphering the selective androgen receptor modulators paradigm". Expert Opinion on Drug Discovery 8 (2): 191–218. February 2013. doi:10.1517/17460441.2013.741582. PMID 23231475.