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AC-262536 is a non-steroidal, tissue-selective androgen receptor (AR) modulator (SARM) that targets AR with high-affinity (pKi = 8.3 vs. 8.9/testosterone), potency (NIH-3T3/MDA-kb2 reporter assay pEC50 = 7.9/8.8 vs. 8.7/8.5/testosterone) and partial agonist activity (Emax = 67% and 72% of testosterone Emax, respectively by NIH-3T3 or MDA-kb2 assay) and high selectivity (no significant affinity for 47 other human nuclear receptors). AC-262536 antagonizes 10 nM DHT-induced LNCaP proliferation (by 47.2% at 100 nM) and prevents castration-induced LH upregulation in rats in vivo (EC50 = 2.8 mg/kg) with greatly reduced adverse effects than testosterone propionate (TP).
Non-steroidal, tissue-selective, potent and highly selective androgen receptor (AR) partial agonist in vitro and in vivo.
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11 - Combustible Solids
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WGK 3
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Charlotte Cutler et al.
Drug testing and analysis, 13(2), 369-385 (2020-09-23)
AC-262536 is one of a number of selective androgen receptor modulators that are being developed by the pharmaceutical industry for treatment of a range of clinical conditions including androgen replacement therapy. Though not available therapeutically, selective androgen receptor modulators are
Fabrice Piu et al.
The Journal of steroid biochemistry and molecular biology, 109(1-2), 129-137 (2008-01-01)
Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial
Tim Sobolevsky et al.
Drug testing and analysis, 13(2), 283-298 (2020-08-28)
In the recent years, a lot of effort was put into the development of multiclass initial testing procedures (ITP) to streamline analytical workflow in antidoping laboratories. Here, a high-throughput assay based on liquid chromatography-triple quadrupole mass spectrometry suitable for use
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