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雷西莫特 /Resiquimod {[allProObj[0].p_purity_real_show]}

货号：A119633 同义名： 雷西莫德 / R848;S28463

Resiquimod（R848）是Toll样受体7和8（TLR7/TLR8）的激动剂，能诱导人类mMDSC成熟为炎性巨噬细胞。

Resiquimod 化学结构 CAS号：144875-48-9
Resiquimod 化学结构
CAS号：144875-48-9
Resiquimod 3D分子结构
CAS号：144875-48-9
Resiquimod 化学结构 CAS号：144875-48-9
Resiquimod 3D分子结构 CAS号：144875-48-9
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Resiquimod 纯度/质量文件 产品仅供科研

货号：A119633 标准纯度： {[allProObj[0].p_purity_real_show]}
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Resiquimod 生物活性

描述 Toll-like receptors (TLRs) are a family of pattern recognition receptors involving in the innate and adaptive immunity. The activation of TLR7, which is intracellular receptor expressed on endosomal membranes, can induce Type 1 interferon and inflammatory response[1]. Resiquimod is an immune system modifier as a TLR7 agonist with high potency induce cytokine expression for the treatment of viral and tumor lesions[2]. The EC50 of the resiquimod is 1.4 μM to TLR7[3].
Acute myeloid leukemia (AML) cells were treated with 5 μg/mL of resiquimod during 24 h. The expression of MHC class I and II molecules on the membrane of primary AML cells measured by flow cytometry and the production of IL-6, IL-1β and TNF-α measured by multiplex fluorescent bead immunoassay, were increased after the treatment with resiquimod[4].
The resiquimod were injected to BALB/c mice with breast cancer intraperitoneally for three continuous days in a week for three weeks. The resiquimod could significantly retard tumor growth compared with the vehicle group by reducing the density of tumor vasculature and inducing tumor cell apoptosis[5].
作用机制 The effect of resiquimod in the TLR signaling pathway is through binding to the TLR7. Therefore, it can activate the TLR7 mainly on dendritic cells, macrophages, and B-lymphocytes.

Resiquimod 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK293 cells Function assay Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601 μM 20232824
HEK293 cells Function assay 24 h Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5 μM 24383475
Huh7 replicon cells Function assay Antiviral activity against HCV infected human Huh7 replicon cells treated with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay 17548497
human PBMC Function assay 24 h Increase in IFNalpha level in human PBMC after 24 hrs relative to control 17548497

Resiquimod 动物研究

Dose C57BL/6 Mice: 1 mg/kg[6] (intratracheally); 2 mg/kg[7] (i.v.) C3H/HeN Mice: 1 mg/kg - 5 mg/kg[8] (i.v.) BALB/c Mice: 3 mg/kg[5] (i.p.) Mice: 10 mg/kg[9] (i.p.), 2 mg/kg[10] (s.c.)
Administration i.v., i.p., s.c.

Resiquimod 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02688478 Allergies Not Applicable Recruiting May 7, 2020 Canada, British Columbia ... 展开 >> University of British columbia Recruiting Vancouver, British Columbia, Canada, V5Z 1M9 Contact: Christopher Carlsten, MD, PHD    604-875-4122    carlsten@mail.ubc.ca    Principal Investigator: Christopher Carlsten, MD, MPH 收起 <<
NCT02637219 - Completed - United States, Washington ... 展开 >> VA Puget Sound Health Care System Seattle, Washington, United States, 98108 收起 <<
NCT02687503 Respiratory Tract Infections Not Applicable Active, not recruiting January 2019 United States, Wisconsin ... 展开 >> UW Health 20 S. Park Clinic Madison, Wisconsin, United States, 53715 UW Health West Towne Clinic Madison, Wisconsin, United States, 53717 收起 <<

Resiquimod 参考文献

[1]Chi H, Li C, Zhao FS, et al. Anti-tumor Activity of Toll-Like Receptor 7 Agonists. Front Pharmacol. 2017.

[2]Meyer T, Surber C, et al. Resiquimod, a topical drug for viral skin lesions and skin cancer. Expert Opin Investig Drugs. 2013;22(1):149-59.

[3]Kubli-Garfias C, Vázquez-Ramírez R, et al. Insights on the mechanism of action of immunostimulants in relation to their pharmacological potency. The effects of imidazoquinolines on TLR8. PLoS One. 2017;12(6):e0178846.

[4]Smits EL, Cools N, et al. The Toll-like receptor 7/8 agonist resiquimod greatly increases the immunostimulatory capacity of human acute myeloid leukemia cells. Cancer Immunol Immunother. 2010;59(1):35-46.

[5]Yin T, He S, Wang Y. Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015;12(3):3515-3520.

Resiquimod 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.90mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL

Resiquimod 技术信息

CAS号144875-48-9
分子式C17H22N4O2
分子量 314.382
别名 雷西莫德 ;R848;S28463;VML-600
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 30 mg/mL(95.43 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 50 mg/mL(159.04 mM)，配合低频超声助溶
动物实验配方

IP 2% DMSO+water 5 mg/mL clear

PO 0.5% CMC-Na 75 mg/mL suspension

Tags: Resiquimod | 144875-48-9 | R848 | S28463 | R 848 | R-848 | S28463 | S 28463 | S-28463 | TLR7/TLR8 Agonist (GMP) | Immunology/Inflammation | Toll-like Receptor (TLR) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Resiquimod 纯度/质量文件 | Resiquimod 生物活性 | Resiquimod 细胞研究 | Resiquimod 动物研究 | Resiquimod 临床数据 | Resiquimod 参考文献 | Resiquimod 实验方案 | Resiquimod 技术信息

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