1357389-11-7
RGFP966(RGFP966)
CAS: 1357389-11-7
化学式: C21H19FN4O
| 中文名 | RGFP966 |
| 英文名 | RGFP966 |
| 别名 | 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 |
| 英文别名 | CS-871 RGFP966 RGFP 966 RGFP-966 RGFP-966 (2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide |
| CAS | 1357389-11-7 |
| 化学式 | C21H19FN4O |
| 分子量 | 362.4 |
| 密度 | 1.19±0.1 g/cm3(Predicted) |
| 沸点 | 630.4±55.0 °C(Predicted) |
| 溶解度 | 溶于DMSO (高达20 mg/ml) |
| 酸度系数 | 11.58±0.70(Predicted) |
| 存储条件 | -20°C |
| 稳定性 | 从提供的购买之日起稳定1年。DMSO中的溶液可以在-20 °C下储存长达1个月。 |
| 外观 | 固体 |
| 颜色 | Off-white |
| 体外研究 | 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. |
| 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. |
| 参考资料 展开查看 | [1]. Malvaez M, et al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52.[2]. Leus NG, et al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74.[3]. Jia H, et al. The Effects of Pharmacological Inhibition of Histone Deacetylase 3 (HDAC3) in Huntington's Disease Mice. PLoS One. 2016 Mar 31;11(3):e0152498.[4]. Bieszczad KM, et al. Histone Deacetylase Inhibition via RGFP966 Releases the Brakes on Sensory Cortical Plasticity and the Specificity of Memory Formation. J Neurosci. 2015 Sep 23;35(38):13124-32. |
1357389-11-7 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.759 ml | 13.797 ml | 27.594 ml |
| 5 mM | 0.552 ml | 2.759 ml | 5.519 ml |
| 10 mM | 0.276 ml | 1.38 ml | 2.759 ml |
| 5 mM | 0.055 ml | 0.276 ml | 0.552 ml |
最后更新：2024-01-02 23:10:35
1357389-11-7 - 细胞实验
Cell lines: HH and Hut78 CTCL cell linesConcentrations: ~10μMIncubation Time: 24 to 72 hMethod: Cells are counted and split into T25 (Corning) flasks at 26105 cells/mL. Cells are then treated with DMSO, or HDIs once at hour 0. 100 ml aliquots are taken in triplicate from each flask at 0 hr, 24 hrs, 48 hrs, and 72 hrs after treatment, distributed into a flat bottom 96-well plate, and 10 ml of alamar blue added to each well. After a 4 hr incubation, fluorescence is measured using the Biotek Synergy MX Microplate Reader.
最后更新：2023-08-16 21:32:38
1357389-11-7 - 动物实验
Animal Models: MouseDosages: 10 mg/kg, 10.0 mL/kgAdministration: s.c.
最后更新：2023-08-16 21:32:38
1357389-11-7 - 简介
RGFP966是一种小分子化合物，通常用作组蛋白去乙酰化酶抑制剂。它是一种具有高度选择性的抑制剂，主要抑制去乙酰化酶4（HDAC4）的活性。
RGFP966可用于研究蛋白去乙酰化修饰在细胞生物学和分子生物学中的作用。它在神经学和心血管学方面的研究中得到广泛应用。RGFP966还被认为具有抗抑郁和记忆增强的潜力。
RGFP966的制法比较简单，一般是通过化学合成的方法得到。具体制法包括一系列化学反应，如芳香环化，取代反应等。
RGFP966可用于研究蛋白去乙酰化修饰在细胞生物学和分子生物学中的作用。它在神经学和心血管学方面的研究中得到广泛应用。RGFP966还被认为具有抗抑郁和记忆增强的潜力。
RGFP966的制法比较简单，一般是通过化学合成的方法得到。具体制法包括一系列化学反应，如芳香环化，取代反应等。
最后更新：2024-04-09 01:59:59
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