store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Resiquimod (R848) 是一种 Toll 样受体7/8的激动剂,可诱导细胞因子上调。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 143 | 现货 | ||
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 452 | 现货 | ||
25 mg | ¥ 725 | 现货 | ||
50 mg | ¥ 1,360 | 现货 | ||
100 mg | ¥ 1,990 | 现货 | ||
200 mg | ¥ 2,680 | 现货 | ||
500 mg | ¥ 3,890 | 现货 | ||
1 g | ¥ 5,570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 523 | 现货 |
产品描述 | Resiquimod (R848) is an imidazoquinoline amine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes. |
体外活性 | Resiquimod induces the differentiation of myeloid-derived suppressor cells into dendritic cells and macrophages and may improve cancer immunotherapy by reducing immunosuppressive MDSCs. Resiquimod activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway [1]. Resiquimod also modulates dendritic cells to augment HIV-1- and cytomegalovirus-specific T cell responses [2]. |
体内活性 | In wild-type mice, Resiquimod (50 nmol, i.p.) promotes increased serum concentrations of TNF-α, IFN-α, and IL-12, while neither MyD88-deficient mice nor TLR7-deficient mice show an increase in these cytokines [1]. In a murine model of allergic asthma, Resiquimod (i.n., 20 μg/mouse) reduces allergen-induced airway reactivity and inflammation via the reduction in Nrf2 signaling. |
激酶实验 | 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. |
细胞实验 | Resiquimod is dissolved in DMSO. 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. |
动物实验 | Animal Models: Wild-type mice,TLR7-deficient mice,and MyD88-deficient mice. Formulation: saline. Dosages: 50 nmol. Administration: i.p. |
别名 | R848, 雷西莫特, S28463 |
化合物与蛋白结合的复合物 |
Crystal structure of human TLR8 in complex with Resiquimod (R848) crystal form 1 |
分子量 | 314.38 |
分子式 | C17H22N4O2 |
CAS No. | 144875-48-9 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 59 mg/mL (187.7 mM)
Ethanol: 20 mg/mL (63.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 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 | |
20 mM | 0.159 mL | 0.7952 mL | 1.5904 mL | 3.9761 mL | |
50 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5904 mL | |
DMSO | 100 mM | 0.0318 mL | 0.159 mL | 0.3181 mL | 0.7952 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Resiquimod 144875-48-9 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HCV Protease TLR Hepatitis C virus R 848 S 28463 R848 R-848 S-28463 Toll-like Receptor (TLR) 雷西莫特 Inhibitor inhibit HCV S28463 inhibitor