| 名稱 | Resiquimod |
| 描述 | Resiquimod (R848) is a Toll-like receptor 7/8 (TLR7/TLR8) agonist that induces cytokine upregulation. Resiquimod is an immunomodulator with antitumor and antiviral activity. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 動(dòng)物實(shí)驗(yàn) | Animal Models: Wild-type mice,TLR7-deficient mice,and MyD88-deficient mice. Formulation: saline. Dosages: 50 nmol. Administration: i.p. |
| 體外活性 | 方法: 金絨球頭腎淋巴細(xì)胞 HKL 用 Resiquimod (0.175-32 μg/mL) 處理 12 h，使用 CCK8 assay 檢測細(xì)胞活力。
結(jié)果: CCK8 測定結(jié)果顯示，0.25-32 μg/mL Resiquimod 顯著促進(jìn) HKL 增殖。[1]
方法: 外周血單核細(xì)胞 PBM 用 Resiquimod (0.01-100 μM) 處理 1-14 h，使用 Western Blot 方法檢測靶點(diǎn)蛋白表達(dá)水平。
結(jié)果: 1 μM 的劑量足以改變 FcγR 的表達(dá)，更高的劑量不會(huì)導(dǎo)致更大的變化。FcγRIIa 的增加發(fā)生在晚期，而 γ 鏈的小幅增加出現(xiàn)在 3 h，但在 14 h 時(shí)更高。然而，F(xiàn)cγRIIb 蛋白在1 h 內(nèi)減少，而 FcγRIIb 的轉(zhuǎn)錄物保持到 4 h。[2] |
| 體內(nèi)活性 | 方法: 為檢測體內(nèi)抗腫瘤活性，將 Resiquimod (2 mg/kg) 和 4D5 抗 HER2 抗體 (20 mg/kg) 腹腔注射給攜帶 CT26-HER2/neu 腫瘤的 Balb/cJ 小鼠，每周三次，持續(xù) 13 天。
結(jié)果: 13 天后，接受 Resiquimod 加抗體的小鼠腫瘤的生長速率顯著降低。統(tǒng)計(jì)測試顯示 4D5 和 Resiquimod 在降低腫瘤生長速率方面具有協(xié)同作用。[2] |
| 存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Saline : 0.1 mg/mL (0.32 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 55 mg/mL (174.95 mM)
Ethanol : 20 mg/mL (63.6 mM)
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| 關(guān)鍵字 | Hepatitis C virus | R 848 | S 28463 | R-848 | S-28463 | Toll-like Receptor (TLR) | Resiquimod | Inhibitor | inhibit | HCV |
| 相關(guān)產(chǎn)品 | Chloranil | Chloroquine phosphate | Honokiol | Hydroxychloroquine | Artemisinin | EIDD-1931 | CU-115 | Methyl 2-amino-5-bromobenzoate | Chloroquine | Deferiprone | Ribavirin | Sofosbuvir |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 抗病毒庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 抗癌藥物庫 |