1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. RGFP966

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)。

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RGFP966 Chemical Structure

RGFP966 Chemical Structure

CAS No. : 1357389-11-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥990
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5 mg ¥900
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10 mg ¥1183
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50 mg ¥4200
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100 mg ¥6120
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 30 篇科研文献

WB
IHC

    RGFP966 purchased from MCE. Usage Cited in: Front Physiol. 2019 Aug 20;10:1060.  [Abstract]

    Osteoarthritis rats are treated with RGFP966. Immunohistochemistry (IHC) was performed to measure relative inflammatory proteins in OA. Expression of collagen II in CG and OAG + RGFP966 group is higher than OAG by IHC.

    RGFP966 purchased from MCE. Usage Cited in: Pancreatology. 2019 Mar;19(2):383-389.  [Abstract]

    RGFP966 decreases PD-L1 expression in a time- and dose-dependent manner in pancreatic cancer cells.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).

    IC50 & Target[1]

    HDAC3

    80 nM (IC50)

    体外研究
    (In Vitro)

    RGFP966 在 RAW 264.7 巨噬细胞中有效且选择性地抑制 HDAC 3,IC50 为 0.21 μM,而 HDACs 1 (IC50=5.6 μM)、2 (9.7 μM) 和 8 (>100 μM),表明对 HDAC 3 具有良好的选择性。HDAC 1、2 和 3 的 mRNA 水平在 RAW 264.7 巨噬细胞中不受 RGFP966 的显著影响,而 HDAC 1 和 HDAC 2 蛋白水平略有影响,尽管在 RGFP966 处理后显著降低。此外,RGFP966 显著降低了 NF-κB p65 的转录活性,而 NF-κB p65 的乙酰化和定位保持不变[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    RGFP966 (10 和 25 mg/kg) 处理显著改善了体重、旋转杆性能和开阔场地运动测试中的多项运动功能指标[3]
    RGFP966 以 10 mg/kg 的剂量穿过血脑屏障进入大鼠听觉皮层,具有典型的药代动力学,这共同证明了由于听觉皮层中的作用而调节 A1 可塑性的可行性[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    362.40

    Formula

    C21H19FN4O

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMF 中的溶解度 : 50 mg/mL (137.97 mM; 超声助溶)

    DMSO 中的溶解度 : 50 mg/mL (137.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7594 mL 13.7969 mL 27.5938 mL
    5 mM 0.5519 mL 2.7594 mL 5.5188 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.90 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.90 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 50% PEG300    50% Saline

      Solubility: 7.69 mg/mL (21.22 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.81%

    参考文献
    Kinase Assay
    [2]

    The respective human recombinant HDAC enzymes are incubated in absence and/or in presence of various concentrations RGFP966 and a pro-fluorogenic substrate at room temperature for 60 min. Next, the deacetylation reaction is stopped by the addition of the HDAC Stop Solution (6 mg/mL trypsin, 0.3 mM SAHA) in all wells and the plate is incubated at 37°C for 20 min. The release of the fluorescent 7-amino-4-methylcoumarin is monitored by measuring the fluorescence at λem=460 nm and λex=390 nm using a Synergy H1 plate reader. The fluorescence value of the background wells is subtracted from the fluorescence of the positive control, blank and inhibitor wells. Nonlinear regression is used to fit the data to the log(inhibitor) vs. response curve using GraphPad Prism[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    To investigate the influence of the HDAC 3-selective inhibitor RGFP966 on cell viability, RAW 264.7 macrophages, HBE cells and hASM cells are seeded in 96-well plates. To obtain identical cell density at the start of the experiments, RAW 264.7 macrophages are seeded at 25,000 cells/cm2, HBE cells and hASM cells are seeded at 70% confluency (based on surface area) and are serum-starved for 24 h prior incubation with RGFP966. Shortly before incubation with RGFP966, the medium is replaced by 100 μL fresh (if appropriate serum free) culture medium. Incubations with LPS and IFNγ are performed as described for HDAC 1-3 downregulation by siRNA. After 20 h of incubation with RGFP966, 20 μL of CellTiter 96 AQueous One Solution reagent is added to each well and incubated at 37°C for 1 h in the dark. The absorbance at 490 nm is measured using a Synergy H1 plate reader. LPS/IFNγ-stimulated cells without addition of RGFP966 are considered 100%[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    N171-82Q transgenic mice are housed and maintained on a normal 12-h light/dark cycle with lights on at 6:00 a.m and free access to food and water. Mice are administered RGFP966 (10 or 25 mg/kg) for 10 weeks by S.C. injection (3 injections/week) beginning at 8 weeks of age. RGFP966 is dissolved with 75% polyethylene glycol 200/25% sodium acetate (6.25 mM); control mice received an equal volume of drug vehicle. Body weights are recorded twice per week. Mice are sacrificed at 18 weeks of age, 6 h after the final injection by overdose with isofluorane anesthesia. Brains are removed, and striata and cortex dissected out for gene expression assays or intracardially perfused with 4% paraformaldehyde.
    Rats[4]
    A total of thirty-three adult male Sprague Dawley rats (275-350 g) are used. Immediately following the daily training session, a posttraining systemic injection of either RGPF966 (10 mg/kg, s.c.) or vehicle (at a comparable volume to drug treatment) is delivered to each subject.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    RGFP966 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMF / DMSO 1 mM 2.7594 mL 13.7969 mL 27.5938 mL 68.9845 mL
    5 mM 0.5519 mL 2.7594 mL 5.5188 mL 13.7969 mL
    10 mM 0.2759 mL 1.3797 mL 2.7594 mL 6.8985 mL
    15 mM 0.1840 mL 0.9198 mL 1.8396 mL 4.5990 mL
    20 mM 0.1380 mL 0.6898 mL 1.3797 mL 3.4492 mL
    25 mM 0.1104 mL 0.5519 mL 1.1038 mL 2.7594 mL
    30 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2995 mL
    40 mM 0.0690 mL 0.3449 mL 0.6898 mL 1.7246 mL
    50 mM 0.0552 mL 0.2759 mL 0.5519 mL 1.3797 mL
    60 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1497 mL
    80 mM 0.0345 mL 0.1725 mL 0.3449 mL 0.8623 mL
    100 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6898 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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