AC-262536 (3, 10, 30 mg/kg) reverses the luteinizing hormone (LH) spike in castrated rats[1]. Animal Model: Male Sprague-Dawley rats (200-225 g)[1] Dosage: 3, 10 and 30 mg/kg Administration: Administered subcutaneously; once daily for 14 consecutive days Result: Significantly decreased LH levels by about 40% at the 3 mg/kg dose. The ED50 was determined to be 2.8 mg/kg. At the 10 and 30 mg/kg doses, the effects of AC-262536 were significantly stronger than Testosterone Propionate (TP) : 1.91±0.32 ng/mL and 1.53±0.34 ng/mL vs. 3.12±0.69 ng/mL, respectively.
In Vitro
AC-262536 dose-dependently inhibits dihydroxytestosterone (DHT)-induced proliferation of LNCaP. The effects are significant with 100 nM AC-262536 (%inhibition 47.2±12.2), and reaches a plateau with 1 μM treatment (%inhibition 50.7±7.6). Thus, AC-262536 can act as a functional antagonist in prostate cells[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Fabrice Piu, et al. Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator. J Steroid Biochem Mol Biol. 2008 Mar;109(1-2):129-37.
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