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Imiquimod

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Chemical Structure| 99011-02-6 同义名 : R 837;S-26308;Beselna.;Vyloma;Zyclara;Imiquimod Brand name: Aldara;TMX 101
CAS号 : 99011-02-6
货号 : A161049
分子式 : C14H16N4
纯度 : 99%+
分子量 : 240.304
MDL号 : MFCD00866946
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: 2 mg/mL(8.32 mM)，配合低频超声，并水浴加热至45℃助溶，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

H2O: 2.5 mg/mL(10.4 mM)，配合低频超声，并调节pH至2
动物实验配方：
生物活性
描述 Toll like receptors (TLR) is a family with ten members that are known to be important for provoking the innate immunity and establishing adaptive immunity[1]. The imiquimod is TLR7 and 8 agonist with EC50 value of 1.5 μM on TLR7[2]. It is effective in treating a variety of primary skin cancers and cutaneous metastases of some malignancies[3].
Imiquimod reduced cell numbers on the DFT1 and DFT2 cells lines in a concentration dependent manner as measured by the WST-8 proliferation assay after incubating with 7.5 - 60 μg/ml of imiquimod for 24 hours. When the cells were incubated with 60 μg/ml of imiquimod for 72 hours, most of cells entered apoptotic pathways and complete apoptosis for all the cells occurred at 120 hours as measured by annexin V and PI staining [4] .
When 30 mg/mouse of imiquimod was applied for seven consecutive days on the back skin of late telogen C57BL/6 mice one day after hair removal, the number of CD45 positive cells increased compared with control group as measure by flow cytometry. The level of IL-6, Cxcl-1, TNF-a, IL23p19 and IL-17a examined by quantitative real-time reverse transcription PCR were induced in the imiquimod treatment group[5].
作用机制 Imiquimod could preferentially bind to TLR7 and to a lesser extent, TLR8[6].
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
NCT00147771 Scleroderma, Localized Phase 3 Completed - Canada, Ontario ... 展开 >> The Hospital for Sick Children Toronto, Ontario, Canada, M5G 1X8 收起 <<
NCT01795313 Ependymoma Not Applicable Recruiting January 2020 United States, Pennsylvania ... 展开 >> Children's Hospital of Pittsburgh of UPMC Recruiting Pittsburgh, Pennsylvania, United States, 15224 Contact: Mary Petrany, RN    412-692-8047    petranym@upmc.edu 收起 <<
NCT00581425 Basal Cell Carcinoma Phase 4 Completed - United States, Texas ... 展开 >> University of Texas Health Science Center of Houston Dermatology Clinic Houston, Texas, United States, 77030 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.16mL

0.83mL

0.42mL

20.81mL

4.16mL

2.08mL

41.61mL

8.32mL

4.16mL
参考文献

[1]Kaisho T, Akira S. Toll-like receptor function and signaling. J Allergy Clin Immunol. 2006;117(5):979-87; quiz 988.

[2]Makarenko EV, Kozlovskiĭ IV. [Comparative characteristics of adenosine triphosphatase activity in the erythrocytes of patients with acute and chronic liver diseases, chronic cholecystitis and in HBs antigen carriers]. Ter Arkh. 1987;59(2):98-100.

[3]Schön MP, Schön M. Imiquimod: mode of action. Br J Dermatol. 2007.

[4]Patchett AL, Darby JM, et al. The Immunomodulatory Small Molecule Imiquimod Induces Apoptosis in Devil Facial Tumour Cell Lines. PLoS One. 2016;11(12):e0168068.

[5]Amberg N, Holcmann M, et al. Effects of Depilation Methods on Imiquimod-Induced Skin Inflammation in Mice. J Invest Dermatol. 2017;137(2):528-531.