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Resiquimod/雷西莫特 {[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触发免疫细胞产生炎症细胞因子，促进自身免疫反应，增强抗原呈递，进而可能导致心肌细胞损伤和功能障碍，引发心肌炎。R848靶向破骨细胞前体并通过 TLR7 抑制它们分化为破骨细胞，诱导 CD34 + 造血祖细胞的髓系分化，包括细胞因子 (IL-1β、TNF-α、IL-6、GM-CSF) 和 CD11c 表面标志物的表达上调。

Resiquimod/雷西莫特 化学结构 CAS号：144875-48-9
Resiquimod/雷西莫特 化学结构
CAS号：144875-48-9
Resiquimod/雷西莫特 3D分子结构
CAS号：144875-48-9
Resiquimod/雷西莫特 化学结构 CAS号：144875-48-9
Resiquimod/雷西莫特 3D分子结构 CAS号：144875-48-9
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Resiquimod/雷西莫特 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/雷西莫特 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].

Resiquimod/雷西莫特 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse splenic B cells 2.5 μg/ml 2 days To determine if T-bet+ B cells secrete CXCL10 protein. Results showed that R848 stimulation significantly increased CXCL10 secretion by B cells compared to medium alone. Cell Metab. 2022 Aug 2;34(8):1121-1136.e6.
U87MG-LTR-Luc cells 10, 20, 40 μM 48 h To test the effect of Resiquimod on HIV-1 LTR transactivation, results showed that Resiquimod could induce HIV-1 LTR transactivation. FASEB J. 2022 Mar;36(3):e22184.

Resiquimod/雷西莫特 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
New Zealand White rabbits Ear inflammation model Subcutaneous injection 5 mg Single injection, observed for 7-10 days Evaluate local immune response and systemic TNF-α secretion of R848-Toco/HA-Toco, showing it induces localized immune responses without systemic inflammation J Control Release. 2019 Jul 28;306:165-176
Mice TLR7 agonist-induced lupus model Intraperitoneal injection 20 mg/kg 3 times per week for 6 weeks To evaluate the effects of 6-gingerol on NET release and autoantibody formation in a lupus mouse model, results showed that 6-gingerol significantly reduced NET levels and autoantibody levels. JCI Insight. 2021 Feb 8;6(3):e138385.
Mice IFN-betaYFP/YFP mice Intraperitoneal injection 50 nM/mouse Single dose 24 hours before imaging To confirm that the IFN-betaYFP/YFP mouse strain was able to report IFN-beta production under stimulation Cells. 2018 Jul 27;7(8):88
Mice Graft-versus-host disease (GvHD) model in B6D2F1 and B6 mice Intraperitoneal injection 25 mg/mouse 48 hours and 24 hours before, or 0 hours before transplantation To evaluate the protective effect of R848 in the GvHD model, results showed that R848 treatment significantly improved survival rates and inhibited inflammatory cytokine production. Haematologica. 2019 Feb;104(2):392-402
Mice Systemic lupus erythematosus model Topical application 100 μg,100 μl Days 0, 2, and 6, for a duration of 10 days To evaluate the effect of the TLR7 agonist R848 on a systemic lupus erythematosus model in mice, showing that R848 treatment increased the frequency of CD69+CD4+ T cells, effector-memory CD4+ T cells, T follicular helper cells, and plasma cells. Sci Adv. 2024 Mar 29;10(13):eadi4310
Mice Normal mice Intraperitoneal injection 50 μg Injected on day 0 and day 2, samples collected on day 4 To investigate the effects of TLR7 agonist R848 on mouse B cells. Results showed that the proportion of T-bet+ CD11c+ B cells was significantly increased in R848-treated mice. Cell Metab. 2022 Aug 2;34(8):1121-1136.e6.
Mice B6.Sle1.Sle2.Sle3 (TC) and TC. Rag1-/- mice Topical application 100 mg,100 mL Three times a week for 2 weeks To assess the effect of TLR7/8 activation on gut integrity, the results showed that R848 increased gut permeability in mice with lupus susceptibility genes but not in non-autoimmune mice. Front Immunol. 2023 Jul 6;14:1187145

Resiquimod/雷西莫特 动物研究

Animal study 心肌炎模型[6-7]
动物：C57BL/6J、FVB/NJ和NOD/ShiLtJ亲本系（CFN系）三重杂交小鼠，雄性或雌性，8~10周龄。
给药：100 μg，右耳皮肤涂抹，每周3次。

Resiquimod/雷西莫特 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/雷西莫特 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.

[6]Hasham MG, Baxan N, Stuckey DJ, et al. Systemic autoimmunity induced by the TLR7/8 agonist Resiquimod causes myocarditis and dilated cardiomyopathy in a new mouse model of autoimmune heart disease. Dis Model Mech. 2017;10(3):259-270.

[7]Yokogawa M, Takaishi M, Nakajima K, et al. Epicutaneous application of toll-like receptor 7 agonists leads to systemic autoimmunity in wild-type mice: a new model of systemic Lupus erythematosus. Arthritis Rheumatol. 2014;66(3):694-706.

Resiquimod/雷西莫特 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/雷西莫特 技术信息

CAS号144875-48-9
分子式C17H22N4O2
分子量 314.38
SMILES Code CC(O)(C)CN1C(COCC)=NC2=C1C3=CC=CC=C3N=C2N
MDL No. MFCD00937759
别名 雷西莫德 ;R848; S28463; VML-600
运输蓝冰
InChI Key BXNMTOQRYBFHNZ-UHFFFAOYSA-N
Pubchem ID 159603
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四

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/雷西莫特 纯度/质量文件 | Resiquimod/雷西莫特 生物活性 | Resiquimod/雷西莫特 动物研究 | Resiquimod/雷西莫特 临床数据 | Resiquimod/雷西莫特 参考文献 | Resiquimod/雷西莫特 实验方案 | Resiquimod/雷西莫特 技术信息

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