产品说明书

Resiquimod

Print
Chemical Structure| 144875-48-9 同义名 : 雷西莫德 ;R848;S28463;VML-600
CAS号 : 144875-48-9
货号 : A119633
分子式 : C17H22N4O2
纯度 : 98%
分子量 : 314.382
MDL号 : MFCD00937759
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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.
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
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 <<
实验方案
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
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.