产品信息
抗原名称
HDAC
商品描述
RGFP966 is specific inhibitor of HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM.
分子量
362.4
纯度
>98%
可溶性
DMSO ：72 mg/mL (198.67 mM)
外观
Powder
In vitro(体外研究)
RGFP966 potently and selectively inhibits HDAC 3 with IC50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC50=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered.
In vivo(体内研究)
RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex.
背景
别名
RGFP966; RGFP-966
分子式
C21H19FN4O
CAS号
1357389-11-7；1396841-57-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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