Description:
IC50 Value: 2.11 ± 0.16 nM (Ki value)[1]
BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator, and this compound has been advanced to clinical trials for the treatment of age-related functional decline. BMS-564929 is a subnanomolar AR agonist in vitro, is highly selective for the AR vs. other steroid hormone receptors, and exhibits no significant interactions with SHBG or aromatase.
in vitro: BMS-564929 is a high affinity ligand for AR with a Ki of 2.11 ± 0.16 nM. This compound is more than 1000-fold selective for AR vs. ERα and β, GR, and MR, and approximately 400-fold selective vs. PR . BMS-564929 exhibited a potency (EC50, calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44 ± 0.03 nM compared with 2.81 ± 0.48 nM measured for T in the C2C12 myoblast cell line [1]. Sample preparation based on solid-phase extraction and subsequent LC-MS/MS measurement allowed for detection limits of 1-20 ng/mL, intra- and interday precisions of between 2.4 and 13.2% and between 6.5 and 24.2%, respectively [2].
in vivo: The compound was administered across a wide dose range (1 μg to 1 mg/kg) for 8 wk in the same recovery schedule of administration as the 2-wk experiments. A dose-dependent increase in levator ani muscle and prostate wet weight was observed with BMS-564929 treatment, with ED50 values of 0.001 and 0.09 mg/kg for the levator ani and prostate, respectively [1]
Clinical trial: N/A