Resiquimod (R-848)

製品コードS8133 バッチS813304

印刷

化学情報

Synonyms

S28463

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₂₂N₄O₂

分子量

314.38

CAS No.

144875-48-9

Solubility (25°C)*

体外

DMSO

63 mg/mL (200.39 mM)

Ethanol (warmed with 50ºC water bath)

63 mg/mL (200.39 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.150mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL 63 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.
in vitro	Resiquimod (R-848) activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway. ^[1] This compound also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses. ^[2] It induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs. ^[3]
in vivo	Resiquimod (R-848) (50 nmol, i.p.) induces increased serum concentrations of IFN-alpha, TNF-alpha and IL-12 in wild-type mice, while neither TLR7-deficient mice nor MyD88-deficient mice show an increase in these cytokines. ^[1] In a murine model of allergic asthma, this compound (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling. ^[4]

製品説明

Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.

in vitro

Resiquimod (R-848) activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway. ^[1]

This compound also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses. ^[2]

It induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs. ^[3]

in vivo

Resiquimod (R-848) (50 nmol, i.p.) induces increased serum concentrations of IFN-alpha, TNF-alpha and IL-12 in wild-type mice, while neither TLR7-deficient mice nor MyD88-deficient mice show an increase in these cytokines. ^[1]

In a murine model of allergic asthma, this compound (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Peripheral blood leukocytes
	濃度	0.5–2 μg/ml
	反応時間	24 h
	実験の流れ	Cells were treated with various concentrations of Resiquimod (R-848).
動物実験	動物モデル	Wild-type mice, TLR7-deficient mice, and MyD88-deficient mice
	投薬量	50 nmol
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/11812998/
https://pubmed.ncbi.nlm.nih.gov/14530357/
https://pubmed.ncbi.nlm.nih.gov/24748512/

https://pubmed.ncbi.nlm.nih.gov/26851512/
https://pubmed.ncbi.nlm.nih.gov/25475963/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Microbiota-driven antitumour immunity mediated by dendritic cell migration [ Nature, 2025, 644(8078):1058-1068]	PubMed: 40659786
Multimodal characterization of the responsiveness of eight hepatitis D virus genotype isolates to interferon-alpha treatment [ J Virol, 2025, e0128025.]	PubMed: 40965142
Regulating Tumor-Associated Macrophage Polarization by Cyclodextrin-Modified PLGA Nanoparticles Loaded with R848 for Treating Colon Cancer [ Int J Nanomedicine, 2024, 19:3589-3605]	PubMed: 38645464
Host-functionalization of macrin nanoparticles to enable drug loading and control tumor-associated macrophage phenotype [ Front Immunol, 2024, 15:1331480]	PubMed: 38545103
Fostamatinib, a Spleen Tyrosine Kinase Inhibitor, Exerts Anti-Inflammatory Activity via Inhibiting STAT1/3 Signaling Pathways [ J Inflamm Res, 2024, 17:9757-9771]	PubMed: 39618932
Reduced Renal CSE/CBS/H2S Contributes to the Progress of Lupus Nephritis [ Biology (Basel), 2023, 12(2)318]	PubMed: 36829595
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909]	PubMed: none
Drug-Dependent Morphological Transitions in Spherical and Worm-Like Polymeric Micelles Define Stability and Pharmacological Performance of Micellar Drugs [ Small, 2022, 18(4):e2103552]	PubMed: 34841670
Investigating Silver Nanoparticles and Resiquimod as a Local Melanoma Treatment [ Eur J Pharm Biopharm, 2022, S0939-6411(2200306-X)]	PubMed: 36549400
Co-ordinated control of the ADP-heptose/ALPK1 signalling network by the E3 ligases TRAF6, TRAF2/c-IAP1 and LUBAC [ Biochem J, 2022, 479(20):2195-2216]	PubMed: 36098982

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。