GTx-007 (S-4) 是具有口服活性的、选择性的非甾体受体雄激素受体 (AR) 调节剂 (SARM) 和部分激动剂,Ki为4 nM。GTx-007 (S-4) 是具有较强活性的、具有组织选择性的 SARM。
GTx-007 (S-4) is only a partial agonist in the prostate and seminal vesicles, restoring them to 33.8 and 28.2% of intact animals, respectively[2].GTx-007 significantly increased uterine expression of Wnt4 and Wnt7a[2].
Resulted in a highly heterogeneous pattern of AR expression in all compartments, with a significant increase of AR-positive cells in the luminal epithelium compared to VC.Had approximately ten glands per uterine cross-section within an endometrium, with a compact stroma, consistent with overall endogenous steroid depletion.Did not detect any impact of GTx-007 on body weight.
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