RGFP966
| 中文名称 | RGFP966 |
|---|---|
| 中文同义词 | (2E)-N-(2-氨基-4-氟苯基)-3-[1-(3-苯基-2-丙烯-1-基)-1H-吡唑-4-基]-2-丙烯酰胺;HDAC3抑制剂(RGFP966);化合物RGFP 966;(E)-N-(2-氨基-4-氟苯基)-3-(1-肉桂基-1H-吡唑-4-基)丙烯酰胺 |
| 英文名称 | RGFP-966 |
| 英文同义词 | RGFP 966;RGFP966;RGFP-966;(2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide;RGFP966, >=98%;(E/Z)-RGFP 966;2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-, (2E)-;CS-871 |
| CAS号 | 1357389-11-7 |
| 分子式 | C21H19FN4O |
| 分子量 | 362.4 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;标准品;Inhibitors |
| Mol文件 | 1357389-11-7.mol |
| 结构式 |  |
RGFP966 性质
| 沸点 | 630.4±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.19±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 可溶于 DMSO（高达 20 mg/ml） |
| 形态 | 固体 |
| 酸度系数(pKa) | 11.58±0.70(Predicted) |
| 颜色 | 米白色 |
| 稳定性 | 可在-20°C下的DMSO溶液保存长达1个月。 |
|
HDAC3 80 nM (IC 50 ) |
RGFP966 potently and selectively inhibits HDAC 3 with IC 50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC 50 =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.
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13909 | RGFP966 RGFP966 | 1357389-11-7 | 5mg | 900元 |
| 2024/01/25 | HY-13909 | RGFP966 RGFP966 | 1357389-11-7 | 10mM * 1mLin DMSO | 990元 |