Resiquimod (R-848)
别名: S28463 中文名称：雷西莫特， 瑞喹莫德
Resiquimod (R-848, S28463)是一种免疫反应调节剂，用作有效的TLR 7/TLR 8激动剂并可诱导如 TNF-α、IL-6 和 IFN-α 等细胞因子的上调。Resiquimod 可减少 hepatitis C virus (HCV)感染。Phase 2。
Resiquimod (R-848) Chemical Structure
CAS: 144875-48-9
客户使用Selleck的发表文献15篇
产品质控
Resiquimod (R-848)相关产品
| 相关靶点 | TLR7 TLR8 TLR9 TLR4 TLR2 TLR3 TLR1 TLR6 | 点击展开 |
|---|---|---|
| 相关产品 | Resatorvid (TAK-242) Motolimod Cu-CPT22 Vesatolimod (GS-9620) TLR2-IN-C29 MD2-IN-1 Lipopolysaccharides IRAK4-IN-2 CU-T12-9 E6446 TLR4-IN-C34 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ | 点击展开 |
TLR抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| PBMC | Function assay | 300 nM | 18 hrs | Induction of type 1 IFN secretion in human PBMC at 300 nM after 18 hrs by ELISA, Activity=0.00726μM. | 20232824 |
| PBMC | Function assay | 100 nM | 18 hrs | Induction of type 1 IFN secretion in human PBMC at 100 nM after 18 hrs by ELISA, Activity=0.00561μM. | 20232824 |
| PBMC | Function assay | 10 nM | 18 hrs | Induction of type 1 IFN secretion in human PBMC at 10 nM after 18 hrs by ELISA, Activity<0.00125μM. | 20232824 |
| PBMC | Function assay | 30 nM | 18 hrs | Induction of type 1 IFN secretion in human PBMC at 30 nM after 18 hrs by ELISA, Activity=0.00125μM. | 20232824 |
| PBMC | Function assay | 1000 nM | 18 hrs | Induction of type 1 IFN secretion in human PBMC at 1000 nM after 18 hrs by ELISA, Activity=0.00775μM. | 20232824 |
| PBMC | Function assay | 22.5 uM | 24 hrs | Agonist activity at TLR7/TLR8 in human PBMC assessed as induction of TNF-alpha production at 22.5 uM after 24 hrs by flow cytometric analysis | 24383475 |
| PBMC | Immunomodulatory assay | 16 uM | 24 hrs | Immunomodulatory activity in human PBMC assessed as induction of IL-6 secretion at 16 uM after 24 hrs by ELISA | 28254484 |
| BMD | Function assay | 1 uM | 48 hrs | Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD86 at 1 uM after 48 hrs by flow cytometry | 19299126 |
| BMD | Function assay | 1 uM | 48 hrs | Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of MHC class-2 at 1 uM after 48 hrs by flow cytometry | 19299126 |
| BMD | Function assay | 1 uM | 48 hrs | Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD40 at 1 uM after 48 hrs by flow cytometry | 19299126 |
| BMD | Function assay | 5 uM | 24 hrs | Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as IL12 production at 5 uM after 24 hrs by ELISA | 19299126 |
| Huh7 | Antiviral assay | 48 hrs | Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced mixed donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.024μM. | 17548497 | |
| Huh7 | Antiviral assay | 48 hrs | Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced single donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.0265μM. | 17548497 | |
| PBMC | Function assay | 24 hrs | Induction of IFNalpha2a level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=0.1μM. | 17548497 | |
| PBMC | Function assay | 24 hrs | Toxic induction of IL1-beta level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. | 17548497 | |
| PBMC | Function assay | 24 hrs | Toxic induction of IL6 level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. | 17548497 | |
| PBMC | Function assay | 24 hrs | Toxic induction of TNFalpha level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. | 17548497 | |
| HEK293 | Function assay | 6 hrs | Agonist activity at human TLR7 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.1μM. | 30143425 | |
| HEK293 | Function assay | 6 hrs | Agonist activity at human TLR8 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.3μM. | 30143425 | |
| HEK | Function assay | 8 to 12 hrs | Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=1.34μM. | 29152046 | |
| HEK | Function assay | 24 hrs | Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=1.4μM. | 22837811 | |
| HEK293 | Function assay | 24 hrs | Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5μM. | 24383475 | |
| HEK293 | Function assay | 6 hrs | Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay, EC50=4μM. | 27270029 | |
| HEK293 | Function assay | 24 hrs | Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=4.5μM. | 24383475 | |
| HEK | Function assay | 8 to 12 hrs | Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=6.13μM. | 29152046 | |
| HEK | Function assay | 24 hrs | Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=6.4μM. | 22837811 | |
| PBMC | Function assay | 24 hrs | Increase in IFNalpha level in human PBMC after 24 hrs relative to control | 17548497 | |
| PBMC | Function assay | 24 hrs | Increase in 2',5'-oligoadenylate synthase level in human PBMC after 24 hrs relative to control | 17548497 | |
| PBMC | Toxicity assay | 24 hrs | Toxicity assessed as increase in IL6 level in human PBMC after 24 hrs relative to control | 17548497 | |
| Huh7 | Antiviral assay | 24 hrs | Antiviral activity against HCV infected human Huh7 replicon cells treated for 24 hrs with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay | 17548497 | |
| HEK293 | Function assay | Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601μM. | 20232824 | ||
| Huh7 | Antiviral 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Resiquimod (R-848, S28463)是一种免疫反应调节剂，用作有效的TLR 7/TLR 8激动剂并可诱导如 TNF-α、IL-6 和 IFN-α 等细胞因子的上调。Resiquimod 可减少 hepatitis C virus (HCV)感染。Phase 2。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Resiquimod激活免疫细胞，并通过Toll-样受体7(TLR7)-MyD88-依赖性信号通路诱导野生型脾细胞的增殖。[1] Resiquimod也会调节树突细胞以增加巨细胞病毒-和HIV-1-特异性T细胞应答。[2] Resiquimod诱导髓源性抑制细胞分化为巨噬细胞和树突细胞，并且可以通过减少免疫抑制的MDSCs提高癌症免疫治疗效果。[3] |
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|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 |
在野生型小鼠中，Resiquimod (50 nmol, i.p.)诱导IFN-α，TNF-α和IL-12的血清浓度增加，而TLR7-缺失或MyD88-缺失的小鼠不会增加其细胞因子。[1] 在过敏性哮喘小鼠模型中，Resiquimod (i.n., 20 μg/小鼠)通过减少Nrf2信号从而减少过敏原诱导的气道反应和炎症。[4] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06021002 | Recruiting | Innate Inflammatory Response|Asthma|Nasal Allergy |
Cambridge University Hospitals NHS Foundation Trust |
August 9 2022 | Not Applicable |
| NCT04127864 | Active not recruiting | Colorectal Cancer|Surgery |
University of Copenhagen|Zealand University Hospital |
October 14 2019 | -- |
| NCT02688478 | Unknown status | Allergies |
University of British Columbia |
February 2 2017 | Not Applicable |
| NCT00960752 | Completed | Melanoma |
M.D. Anderson Cancer Center |
May 20 2010 | Phase 2 |
化学信息&溶解度
| 分子量 | 314.38 | 分子式 | C17H22N4O2 |
| CAS号 | 144875-48-9 | SDF | Download Resiquimod (R-848) SDF |
| Smiles | CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 62 mg/mL ( (197.21 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 51 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
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Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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