AC-262536，50MG，SML3278-50MG，Sigma

Biochem/physiol Actions

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.