Home>>Signaling Pathways>> Microbiology & Virology>> HCV>>Resiquimod (R-848)

Resiquimod (R-848) Sale

(Synonyms: 雷西莫特; R848; S28463) 目录号 : GC13650

Resiquimod (R848) is an imidazoquinoline compound with potential antiviral activity.

Resiquimod (R-848) Chemical Structure

Cas No.:144875-48-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥594.00
现货
10mg
¥540.00
现货
25 mg
¥990.00
现货
50mg
¥1,530.00
现货
100mg
¥2,160.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

客户使用产品发表文献 2

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

Native mast cells

Preparation Method

The purified mast cells were incubated with medium alone or Resiquimod at a final concentration of 10 g/ml for 6 or 12 h at 37℃ in a humidified atmosphere with 5% CO2.

Reaction Conditions

10 µg/ml Resiquimod; 6 or 12 h

Applications

Resiquimod induced the increase of high-affinity IgE receptor (FcεRI) expression.

Animal experiment [2]:

Animal models

Female BALB/c mice

Preparation Method

Mice were inoculated subcutaneously with 4T1 cells. At day 6 after inoculation, mice were treated with vehicle (6% dimethyl sulfoxide + 94% normal saline) and Resiquimod [3 mg/kg, intraperitoneally (IP)] (n=5/group).

Dosage form

3 mg/kg Resiquimod;i.p ; three continuous days in a week for three weeks.

Applications

Resiquimod exhibits antitumoral effects in a murine breast cancer model.

References:

[1].Agier J, Brzezińska-Błaszczyk E,et,al.he impact of TLR7 agonist R848 treatment on mast cell phenotype and activity. Cell Immunol. 2021 Jan;359:104241. doi: 10.1016/j.cellimm.2020.104241. Epub 2020 Oct 28. PMID: 33158544.
[2].Yin T, He S,et,al. Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015 Sep;12(3):3515-3520. doi: 10.3892/mmr.2015.3885. Epub 2015 Jun 3. PMID: 26043701.

产品描述

Resiquimod (R848) is an imidazoquinoline compound with potential antiviral activity. It is a low molecular weight synthetic molecule that has been evaluated in clinical studies for the treatment of infections caused by viruses such as herpes simplex virus and hepatitis C virus[1]. Resiquimod was found to reduce viral shedding and viral reoccurrence by activating various immune cells to produce an environment conductive for the T-helper 1 (Th1) immune responses[2-3]. Resiquimod is a selective ligand for Toll-like receptor (TLR) 7 in mouse and for TLR7 and TLR8 in human and has been shown to activate only TLR7 and TLR8[4].

Resiquimod(10 µg/ml; 6 or 12 h) induced the increase of high-affinity IgE receptor (FcεRI) expression in native mast cells [5].

Resiquimod 8(3 mg/kg;i.p ; three continuous days in a week for three weeks) exhibited a robust antitumoral effect. Resiquimod reduced tumor vasculature and induced tumor cell apoptosis. Resiquimod increased high mobility group Box 1 expression in tumor tissues and activated CD4+ T cells in the peripheral blood[6]. Resiquimod (10 g; i.p) induces anti-tumor responses and attenuates cachexia in murine models of pancreatic ductal adenocarcinoma (PDAC)[7]. The combination of Resiquimod (3 mg/kg were administered by retro-orbital injections (diluted in PBS, 100 µL per mouse) 1 day before, 1 day after, and 1 week after SBRT treatments (total of 3 times))and SBRT results in significant immune activation of the pancreatic tumor microenvironment (TME), including increased tumor antigen-specific CD8+ T cells, decreased regulatory T cells, and enhanced antigen-presenting cells maturation, as well as increased interferon gamma, granzyme B, and CCL5 along with decreased levels of interleukin 4 (IL-4), IL-6, and IL-10[8].

Resiquimod (R848)是一种具有潜在抗病毒活性的咪唑喹啉类化合物。它是一种低分子量的合成分子,在临床研究中已被评价用于治疗单纯疱疹病毒、丙型肝炎病毒等病毒引起的感染[1]。R848被发现通过激活各种免疫细胞产生有利于t -辅助性1 (Th1)免疫应答的环境来减少病毒脱落和病毒复发[2-3]。R848是小鼠toll样受体(TLR) 7和人类TLR7和TLR8的选择性配体(激动剂) [4]

在肥大细胞中,Resiquimod (10µg/ml;6/12 h)诱导高亲和IgE受体(FcεRI)表达升高[5]。

Resiquimod (3 mg/kg;i.p ; three continuous days in a week for three weeks)表现出强大的抗肿瘤作用。Resiquimod减少肿瘤血管,诱导肿瘤细胞凋亡。Resiquimod增加肿瘤组织中高迁移率族蛋白Box1的表达,激活外周血中CD4+ T细胞[6]。Resiquimod (10 g; i.p)在胰腺导管腺癌(PDAC)小鼠模型中诱导抗肿瘤反应并减轻恶病质[7]。Resiquimod (3 mg/kg were administered by retro-orbital injections (diluted in PBS, 100 µL per mouse) 1 day before, 1 day after, and 1 week after SBRT treatments (total of 3 times))和SBRT联合使用导致胰腺肿瘤微环境显著的免疫激活,包括肿瘤抗原特异性CD8+ T细胞增加,调节性T细胞减少,抗原提呈细胞成熟增强,干扰素γ、颗粒酶B和CCL5增加,白细胞介素4 (IL-4)、IL-6和IL-10水平降低[8]。

References:
[1]. Miller RL, Meng TC,et,al. The antiviral activity of Toll-like receptor 7 and 7/8 agonists. Drug News Perspect. 2008 Mar;21(2):69-87. doi: 10.1358/dnp.2008.21.2.1188193. PMID: 18389099.
[2]. Bernstein DI, Harrison CJ, ,et,al. Daily or weekly therapy with resiquimod (R-848) reduces genital recurrences in herpes simplex virus-infected guinea pigs during and after treatment. J Infect Dis. 2001 Mar 15;183(6):844-9. doi: 10.1086/319262. Epub 2001 Feb 13. PMID: 11237799.
[3]. Wu JJ, Huang DB,et,al. Resiquimod: a new immune response modifier with potential as a vaccine adjuvant for Th1 immune responses. Antiviral Res. 2004 Nov;64(2):79-83. doi: 10.1016/j.antiviral.2004.07.002. PMID: 15498602.
[4]. Heil F, Hemmi H,et,al. Species-specific recognition of single-stranded RNA via toll-like receptor 7 and 8. Science. 2004 Mar 5;303(5663):1526-9. doi: 10.1126/science.1093620. Epub 2004 Feb 19. PMID: 14976262.
[5]. Agier J, Brzezińska-Błaszczyk E,et,al. The impact of TLR7 agonist R848 treatment on mast cell phenotype and activity. Cell Immunol. 2021 Jan;359:104241. doi: 10.1016/j.cellimm.2020.104241. Epub 2020 Oct 28. PMID: 33158544.
[6]. Yin T, He S,et,al.Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015 Sep;12(3):3515-3520. doi: 10.3892/mmr.2015.3885. Epub 2015 Jun 3. PMID: 26043701.
[7]. Michaelis KA, Norgard MA,et,al. The TLR7/8 agonist R848 remodels tumor and host responses to promote survival in pancreatic cancer. Nat Commun. 2019 Oct 15;10(1):4682. doi: 10.1038/s41467-019-12657-w. Erratum in: Nat Commun. 2019 Nov 15;10(1):5257. PMID: 31615993; PMCID: PMC6794326.
[8]. Ye J, Mills BN,et,al. Toll-like receptor 7/8 agonist R848 alters the immune tumor microenvironment and enhances SBRT-induced antitumor efficacy in murine models of pancreatic cancer. J Immunother Cancer. 2022 Jul;10(7):e004784. doi: 10.1136/jitc-2022-004784. PMID: 35851308; PMCID: PMC9295644.

Chemical Properties

Cas No. 144875-48-9 SDF
别名 雷西莫特; R848; S28463
化学名 1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol
Canonical SMILES CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N
分子式 C17H22N4O2 分子量 314.38
溶解度 ≥ 33.8 mg/mL in EtOH with ultrasonic, ≥ 1.62 mg/mL in Water with ultrasonic and warming; 30 mg/mL in DMSO (Need ultrasonic) 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
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
10 mM 0.3181 mL 1.5904 mL 3.1809 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置