RGFP 966
RGFP966
CAS: 1357389-11-7
Molecular Formula: C21H19FN4O
RGFP 966 - Names and Identifiers
| Name | RGFP966 |
| Synonyms | 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 |
RGFP 966 - Physico-chemical Properties
| Molecular Formula | C21H19FN4O |
| Molar Mass | 362.4 |
| Density | 1.19±0.1 g/cm3(Predicted) |
| Boling Point | 630.4±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| Appearance | solid |
| Color | Off-white |
| pKa | 11.58±0.70(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Use | RGFP966 is a selective HDAC3 inhibitor . S ystemic treatment with RGFP966 facilitates extinction in mice in a manner resistant to reinstatement. A single treatment of RGFP966 enhances extinction of a previously established cocaine-conditioned place preference, while simultaneously enhancing long-term object-location memory within subjects. During extinction consolidation, HDAC3 inhibition promotes a distinct pattern of histone acetylation linked to gene expression within the infralimbic cortex, hippocampus, and nucleus accumbens. Thus, the facilitated extinction of drug-seeking cannot be explained by adverse effects on performance. |
| In vitro study | 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. |
| In vivo study | 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. |
RGFP 966 - Reference
| Reference Show more | [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. |
RGFP 966 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
RGFP 966 - Cell Experiment
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.
Last Update：2023-08-16 21:32:38
RGFP 966 - Animal Experiment
Animal Models: MouseDosages: 10 mg/kg, 10.0 mL/kgAdministration: s.c.
Last Update：2023-08-16 21:32:38
RGFP 966 - Reference Information
| biological activity | RGFP966 is a highly selective HDAC3 inhibitor with IC50 of 80 nM and no inhibitory effect on other HDACs at 15 μM. RGFP966 can penetrate the blood-brain barrier (BBB). |
| target | HDAC3 80 nM (IC 50 ) |
| in vitro study | RGFP966 potently and selectively inhibits HDAC 3 with IC 50 of 0.21 μ m in RAW 264.7 macrophages, while HDACs 1 (IC 50=5.6 μ m), 2 (9.7 μ m) and 8 (>100 μ m), 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 study | 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. |
Last Update：2024-04-09 01:59:59
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Spot supply
Product Name: RGFP966 Visit Supplier Webpage Request for quotationCAS: 1357389-11-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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