A selective androgen receptor modulator
AC-262536 is a selective androgen receptor modulator (SARM; Ki = 5.01 nM).1 It is also a partial agonist of the androgen receptor (EC50 = 1.58 nM in a luciferase assay). AC-262536 is selective for the androgen receptor over a panel of 47 additional human nuclear receptors at 10 µM. It inhibits dihydroxytestosterone-induced proliferation of LNCaP prostate cancer cells when used at concentrations of 0.1 and 1 µM. AC-262536 (3, 10, and 30 mg/kg) reduces plasma luteinizing hormone levels and increases levator ani muscle weight, a marker of anabolic activity, in castrated rats. It exhibits smaller increases in prostate gland and seminal vesicle weight, markers of androgenic activity, compared with testosterone in the same model.
1.Piu, F., Gardell, L.R., Son, T., et al.Pharmacological characterization of AC-262536, a novel selective androgen receptor modulatorJ. Steroid Biochem. Mol. Biol.109(1-2)129-137(2008)
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