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    Resiquimod (R848)
    Resiquimod (R848)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1867
    CAS #: 144875-48-9Purity ≥98%

    Description: Resiquimod (formerly known as R-848; S-28463; VML-600; R848, S27609) is a potent imidazoquinolinamine-based immune response modifier that acts as an agonist of the TLR 7/8 receptors (Toll-like receptor 7/8) with antiviral and antitumour activity. It can induce the levels of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod is the analogue of imiquimod (also called R-837,S-26308) with potential immunostimulatory activity. Resiquimod has been reported to dose-dependently induce cytokines including IFN, TNF, IL-1β and IL-6 in human peripheral blood mononuclear (PBMCs). In addition, Resiquimod has been revealed to stimulate intracellular IL-1β increased approximately 15%. The results have also been noted that both monocytes and B cells produced IFN in response to Resiquimod. On April 28, 2016, orphan designation (EU/3/16/1653) was granted by the European Commission to resiquimod for the treatment of cutaneous T-cell lymphoma.

    References: Nat Immunol. 2002 Feb;3(2):196-200; J Immunol. 2003 Oct 15;171(8):4320-8.


    Publications Citing Use of InvivoChem Resiquimod (R848)Iran J Immunol. 2022 Mar;19(1):6. doi: 10.22034/IJI.2022.92576.2155.


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    Molecular Weight (MW)314.38 
    FormulaC17H22N4O2 
    CAS No.144875-48-9 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 63 mg/mL (200.4 mM) 
    Water: <1 mg/mL
    Ethanol: 21 mg/mL (66.8 mM) 
    SMILES CodeCC(O)(C)CN1C(COCC)=NC2=C1C3=CC=CC=C3N=C2N
    SynonymsR-848; S-28463; VML600; R848; S 28463; VML 600; R 848; S28463; VML-600.


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    In Vitro

    In vitro activity: Resiquimod activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway. Resiquimod also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses. Resiquimod induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs.


    Kinase Assay: 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. 


    Cell Assay: Unlike LPS-induced activation, which was MyD88-independent, Resiquimod-induced activation of NF-κB was completely dependent on MyD88. It was implied that Resiquimod activated macrophages via TLRs.

    In VivoIn wild-type mice, Resiquimod (50 nmol, i.p.) induces increased serum concentrations of IFN-alpha, TNF-alpha and IL-12, while neither TLR7-deficient mice nor MyD88-deficient mice show an increase in these cytokines. In a murine model of allergic asthma, Resiquimod (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling. 
    Animal modelWild-type mice, TLR7-deficient mice, and MyD88-deficient mice
    Formulation & DosageDissolved in saline; 50 nmol; i.p. injection 
    ReferencesNat Immunol. 2002 Feb;3(2):196-200; J Immunol. 2003 Oct 15;171(8):4320-8. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Resiquimod (formerly known as R-848; S-28463; VML-600; R848, S27609) is a potent imidazoquinolinamine-based immune response modifier that acts as an agonist of the TLR 7/8 receptors (Toll-like receptor 7/8) with antiviral and antitumour activity.

    Resiquimod (R848)

    Both PDCs and MDCs cultured in the presence of the appropriate TLR ligands stimulate higher percentages of responding Ag-specific CD4+ T cells compared with monocytes and B cells. A, Bar graph shows frequencies of CMV-specific CD4+ T cells producing IFN-γ, IL-2, and/or TNF-α when activated by the APC subsets exposed to CMV Ags in addition to the indicated TLR ligands in one representative donor. B, The flow graphs illustrate cytokine production in responding CD3+ T cells stimulated by R-848-exposed and unexposed APCs from another donor. The displayed data in B represent gated CD3+ T cells.

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