1. 诱导疾病模型产品 Immunology/Inflammation Anti-infection
  2. 免疫与炎症疾病模型 心血管系统疾病模型 Toll-like Receptor (TLR) HCV
  3. 心肌炎模型 心脏疾病模型
  4. Resiquimod

Resiquimod  (Synonyms: 雷西莫特; R848; S28463)

目录号: HY-13740 纯度: 99.77%
COA 产品使用指南

Resiquimod是一种Toll样受体7和8 (TLR7/TLR8) 的激动剂, 诱导细胞因子如TNF-α,IL-6和IFN-α的上调。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Resiquimod Chemical Structure

Resiquimod Chemical Structure

CAS No. : 144875-48-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660
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5 mg ¥375
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10 mg ¥600
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25 mg ¥1100
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50 mg ¥1700
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100 mg ¥2400
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500 mg ¥4700
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 51 篇科研文献

Proliferation Assay
RT-PCR
WB

    Resiquimod purchased from MCE. Usage Cited in: Cancer Gene Ther. 2023 Feb 13.  [Abstract]

    Resiquimod (10-200 μM) reduces E-cadherin and Wnt5a expression in a dose-dependent manner.

    Resiquimod purchased from MCE. Usage Cited in: Cytokine. 2017 Nov;99:310-315.  [Abstract]

    IL-23 production by macrophages after stimulation with LPS or Resiquimod M1 macrophages (day 9) were stimulated with LPS (10 ng) or Resiquimod (5 μM) for 6 h and IL-23 protein is measured by ELISA.

    Resiquimod purchased from MCE. Usage Cited in: J Interferon Cytokine Res. 2016 Sep;36(9):563-72.  [Abstract]

    With the stimulus of agonists LPS, ODN2006, Poly (I: C), and R848, the mRNA levels of goOASL in PBMCs are significantly upregulated in LPS- and Poly (I: C)-treated groups, and extremely upregulated in ODN2006- and R848-treated groups.

    查看 Toll-like Receptor (TLR) 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.

    IC50 & Target

    TLR7

     

    TLR8

     

    体外研究
    (In Vitro)

    Resiquimod (R-848) 诱导半抗原和过敏原特异性循环 T 细胞 (包括 TH2 效应子) 产生 IFN-γ,甚至丧失产生 IL-4 的能力[2]
    Resiquimod (R848) 以剂量依赖性方式增强 PBL 增殖,并增加 BrdU 掺入试验中 BrdU 阳性细胞的数量。用 R848 处理的细胞表现出显著增加 (3.5 倍) 的荧光素酶 (NF-κB 活性的报告分子) 活性[3]

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

    体内研究
    (In Vivo)

    Resiquimod 可用于动物建模,构建大小鼠细胞因子释放模型、免疫介导的心脏组织损伤模型。

    Resiquimod (R-848) (50 μg/只,肌肉注射途径) 显著上调在 SPF 鸡中 IFN-α、IFN-β、IFN-γ、IL-1β、IL-4、iNOS 和 MHC-II 基因的表达[1]
    Resiquimod 的药代动力学特性的特点是半衰期短,导致相关剂量下的 AUC 较低,同时 Cmax 较高[5]

    1. 诱导系统性红斑狼疮模型[4]
    致病原理
    TLR 信号传导的改变会导致人类和小鼠模型中狼疮的发生和/或恶化。自身反应性 B 细胞(其中 TLR-7 激活响应含 RNA 的抗原而发生)与 B 细胞受体协同作用,经历增殖、同种型转换和浆细胞分化,导致自身抗体的产生。
    具体造模方法
    Mice: Wild-type FVB/N, BALB/c, and C57BL/6 mice?• female?• 7-9 weeks old (period: 4 weeks)
    Administration: 100 μg?• topical application to the right ear?•?three times a week for 4 weeks.
    Note
    配制:100 μg Resiquimod 溶于 100 μL 丙酮中。
    造模成功指标
    代谢变化:出现全身性自身免疫性疾病,双链 DNA 自身抗体水平升高,多器官受累,包括肾小球肾炎、肝炎、心脏炎。
    组织学分析:脾脏明显肿大,肝脏门静脉周围严重单核细胞浸润,肝细胞坏死。
    相关产品 Myosin H Chain Fragment, mouse (HY-P2464)
    拮抗产品Enpatoran (HY-134581)

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

    Clinical Trial
    分子量

    314.38

    Formula

    C17H22N4O2

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    瑞喹莫德;雷西莫特;雷西喹莫特

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMF 中的溶解度 : 50 mg/mL (159.04 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 30 mg/mL (95.43 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Methanol 中的溶解度 : 25 mg/mL (79.52 mM; 超声助溶)

    H2O 中的溶解度 : 0.1 mg/mL (0.32 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.1809 mL 15.9043 mL 31.8086 mL
    5 mM 0.6362 mL 3.1809 mL 6.3617 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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (7.95 mM); 澄清溶液

    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (6.62 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。
    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: 99.95%

    参考文献
    Kinase Assay
    [3]

    For luciferase assay, FG-9307 cells are transfected with the firefly NF-κB-specific luciferase reporter vector pNFκB-Met-Luc2. Transfection efficiency is monitored by co-transfection with the pSEAP2 control vector, which constitutively expresses the human secreted enhanced alkaline phosphatase (SEAP). Then the cells are treated with Resiquimod (R848, 1 µg/mL), CQ (10 µM), CQ plus R848 or PBS and incubated at 22°C for 24 h. The culture medium of the transfectants is then analyzed for luciferase activity and SEAP activity using Luciferase Assay Kit and the Great EscAPe™ SEAP Chemiluminescence Detection Kit, respectively. The assay is performed three times.

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

    Cell Assay
    [3]

    For inhibition of lysosomal acidification, cells are incubated with 10 µM CQ for 1 h before Resiquimod (R848) treatment. After treatment, 20 µL of 5 mg/mL MTT is added to the plate. The plate is incubated at 22°C for 4 h, and 200 µL dimethyl sulfoxide is added to the plate to dissolve the reduced formazan. The plate is then read at 490 nm with a microplate reader. To determine the effect of Myd88 inhibition on R848-induced cell proliferation, the Myd88 inhibitor Pepinh-MYD and the control peptide Pepinh-Control are added to PBL at the concentration of 50 µM, and the plate is incubated at 22°C for 6 h. After incubation, the cells are treated with R848 and subjected to MTT assay as above. To determine the effect of NF-κB inactivation on R848-induced cell proliferation, BAY-11-7082, an irreversible inhibitor of IκB-α phosphorylation, is added to the cells at the concentration of 1 µM, and the plate is incubated at 22°C for 1 h. After incubation, the cells are treated with R848 and subjected to MTT assay as earlier. All experiments are performed three times.

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

    Animal Administration
    [1]

    A total of 40 SPF chickens of two-week old are allotted to one of the following four experimental groups (n=10/group): Group A: PBS control; Group B: inactivated NDV vaccine; Group C: commercial oil adjuvanted inactivated NDV vaccine prepared from lentogenic strain and Group D: combination of inactivated NDV vaccine and R-848 (50 μg/bird). Vaccine or PBS is administered by intramuscular route in the thigh muscle. A booster dose is given 14-day post immunization (d.p.i). Two weeks post-booster, experimental SPF birds are challenged with velogenic strain of NDV (105 ELD50 per bird) intramuscularly. Clinical signs and mortality are observed daily till 14 day post-challenge (d.p.c). Cloacal swabs (n=6/group) are collected from the birds on day 0, 4, 7 and 14 post-challenge and inoculated into 10-day old embryonated chicken eggs (n=3 eggs/sample) through intra-allantoic route. Three day post-inoculation, the allantoic fluid is checked for the NDV growth by spot haemagglutination using 10% chicken RBC.

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

    参考文献

    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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6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
    Methanol / DMSO / DMF 1 mM 3.1809 mL 15.9043 mL 31.8086 mL 79.5216 mL
    5 mM 0.6362 mL 3.1809 mL 6.3617 mL 15.9043 mL
    10 mM 0.3181 mL 1.5904 mL 3.1809 mL 7.9522 mL
    15 mM 0.2121 mL 1.0603 mL 2.1206 mL 5.3014 mL
    20 mM 0.1590 mL 0.7952 mL 1.5904 mL 3.9761 mL
    25 mM 0.1272 mL 0.6362 mL 1.2723 mL 3.1809 mL
    30 mM 0.1060 mL 0.5301 mL 1.0603 mL 2.6507 mL
    40 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9880 mL
    50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5904 mL
    60 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3254 mL
    DMSO / DMF 80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9940 mL
    DMF 100 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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