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编 号:F182267
分子式:C14H13F3N2O2S
分子量:330.33
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.

体外研究:
GSK-2881078 对雄激素可诱导的酵母和 PC3(AR)2 细胞 (人前列腺癌细胞) 报告基因的 EC50 分别为 4.44 μM 和 3.99 × 10?3 μM。GSK-2881078 (10?5-10 μM, 24 h) 剂量依赖性地刺激 PC3(AR)2 中报告基因的表达,使相对发光单位从 140% 提升到 17340% 。
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