RGFP966
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- CAS号:
- 1357389-11-7
- 英文名:
- RGFP-966
- 英文别名:
- CS-871;RGFP966;RGFP-966;RGFP 966;(E/Z)-RGFP 966;RGFP966, >=98%;RGFP966; RGFP-966;(2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide;2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-, (2E)-
- 中文名:
- RGFP966
- 中文别名:
- 化合物RGFP 966;HDAC3抑制剂(RGFP966);(E)-N-(2-氨基-4-氟苯基)-3-(1-肉桂基-1H-吡唑-4-基)丙烯酰胺;(2E)-N-(2-氨基-4-氟苯基)-3-(1-(3-苯基烯丙基)-1H-吡唑-4-基)丙烯酰胺;(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
- CBNumber:
- CB62666682
- 分子式:
- C21H19FN4O
- 分子量:
- 362.4
- MOL File:
- 1357389-11-7.mol
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RGFP966化学性质
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沸点:
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630.4±55.0 °C(Predicted)
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密度:
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1.19±0.1 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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Soluble in DMSO (up to 20 mg/ml)
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形态:
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solid
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酸度系数(pKa):
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11.58±0.70(Predicted)
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颜色:
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Off-white
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稳定性:
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Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
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RGFP966性质、用途与生产工艺
RGFP966 是高选择性的 HDAC3 抑制剂，IC50 为 80 nM，在 15 μM 时对其他 HDAC 无抑制作用。RGFP966 能够透过血脑屏障 (BBB)。
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.
RGFP966
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-13909 | RGFP966
RGFP966 | 1357389-11-7 | 5mg | 900元 |
| 2024/08/19 | HY-13909 | RGFP966
RGFP966 | 1357389-11-7 | 10mM * 1mLin DMSO | 990元 |
1357389-11-7, RGFP966 相关搜索:
- Inhibitors
- 标准品
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- (2E)-N-(2-氨基-4-氟苯基)-3-(1-(3-苯基烯丙基)-1H-吡唑-4-基)丙烯酰胺
- (E)-N-(2-氨基-4-氟苯基)-3-(1-肉桂基-1H-吡唑-4-基)丙烯酰胺
- 化合物RGFP 966
- HDAC3抑制剂(RGFP966)
- (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
- 1357389-11-7
- RGFP966; RGFP-966
- CS-871
- 2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-, (2E)-
- (E/Z)-RGFP 966
- RGFP966, >=98%
- (2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide
- RGFP-966
- RGFP966
- RGFP 966