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Resiquimod

产品编号 T6964 CAS 144875-48-9

别名: R848, 雷西莫特, S28463

Resiquimod (R848) 是一种 Toll 样受体7/8的激动剂，可诱导细胞因子上调。

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Resiquimod, CAS 144875-48-9

规格	价格/CNY	货期
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

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选择批次

纯度: 99.95%

纯度: 99.92%

纯度: 99.78%

纯度: 99.73%

纯度: 99.67%

纯度: 99.62%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 59 mg/mL (187.7 mM)

Ethanol: 20 mg/mL (63.6 mM)

溶液配制表

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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Hemmi H, et al. Nat Immunol. 2002, 3(2), 196-200. 2. Loré K, et al. J Immunol. 2003, 171(8), 4320-4328. 3. Lee M, et al. Arch Pharm Res. 2014, 37(9), 1234-1240. 4. Nadeem A, et al. Int J Biochem Cell Biol. 2016, 73, 53-62. 6. Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8-induced, Myd88- and NF-κB-dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113-20. 7. Gao Y, Wang K, Wang P, et al. A novel network pharmacology strategy to decode mechanism of Lang Chuang Wan in treating systemic lupus erythematosus[J]. Frontiers in Pharmacology . 2020, 11.

文献引用

1. Gao Y, Wang K, Wang P, et al A novel network pharmacology strategy to decode mechanism of Lang Chuang Wan in treating systemic lupus erythematosus. Frontiers in Pharmacology. 2020, 11.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

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

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Resiquimod

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords