R-848 is a selective ligand for Toll-like receptor 7 (TLR7) in mouse and for TLR7 and TLR8 in human. Potent antitumor and antiviral compound. Stimulates antibody secretion, cytokine production, protection from apoptosis and CD80 upregulation.
Product Specification
| Alternative Name: | 4-Amino-2-(ethoxymethyl)-a,a-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol, S 28463, Resiquimod |
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| Formula: | C17H22N4O2 |
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| MW: | 314.4 |
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| Source: | Synthetic |
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| CAS: | 144875-48-9 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Identity determined by MS, 1H-NMR and 13C-NMR. |
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| Endotoxin Content: | Endotoxin-free |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO, dichloromethane, 100% or 5% methanol; poorly soluble in acetonitrile or ethyl acetate. |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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A Solid-in-Oil Nanodispersion System for Transcutaneous Immunotherapy of Cow's Milk Allergies: M. Kitaoka, et al.; Pharmaceutics
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Acute Conditioning of Antigen-Expanded CD8 + T Cells via the GSK3β-mTORC Axis Differentially Dictates Their Immediate and Distal Responses after Antigen Rechallenge: P. Taborska, et al.; Cancers
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Anti-neutrophil properties of natural gingerols in models of lupus: R.A. Ali, et al.; JCI Insight
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The TLR7 ligand R848 prevents mouse graft-versus-host disease and cooperates with anti-interleukin-27 antibody for maximal protection and regulatory T-cell upregulation: M. Gaignage, et al.; Haematologica
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The TLR7/8 agonist R848 remodels tumor and host responses to promote survival in pancreatic cancer: K.A. Michaelis, et al.; Nat. Commun.
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Assessment of lung cell toxicity of various gasoline engine exhausts using a versatile in vitro exposure system: C. Bisig, et al.; Environ. Pollut.
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N-methyl-D-aspartate receptor antibody production from germinal center reactions: Therapeutic implications: M. Makuch, et al.; Ann. Neurol.
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Polymer-based nanoparticles loaded with a TLR7 ligand to target the lymph node for immunostimulation: J. Widmer, et al.; Int. J. Pharm.
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Adjuvanting an SIV vaccine with TLR ligands encapsulated in nanoparticles induces persistent antibody responses and enhanced protection in TRIM5α restrictive macaques: S.P. Kasturi, et al.; J. Virol.
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Ly6C+ monocyte efferocytosis and cross-presentation of cell-associated antigens: S.R. Larson, et al.; Cell Death Differ.
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Application(s): Efferocytosis assay, in vivo studies,
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Full Text
NLRP3 activation and mitosis are mutually exclusive events coordinated by NEK7, a new inflammasome component: H. Shi, et al.; Nat. Immunol.
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Application(s): Stimulation of human monocytes,
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Notch-Hes-1 axis controls TLR7-mediated autophagic death of macrophage via induction of P62 in mice with lupus: X. Li, et al.; Cell Death Dis.
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Toll-like receptor 3 adjuvant in combination with virus-like particles elicit a humoral response against HIV: E. Poteet, et al.; Vaccine
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A porcine reproductive and respiratory syndrome virus (PRRSV) vaccine candidate based on the fusion protein of PRRSV glycoprotein 5 and the Toll-like Receptor-5 agonist Salmonella Typhimurium FljB: D. Xiong, et al.; BMC Vet. Res.
11, 121 (2015),
Application(s): Intraperitoneal Immunization,
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Evaluation of a biodegradable microparticulate polymer as a carrier for Burkholderia pseudomallei subunit vaccines in a mouse model of melioidosis: K.L. Schully, et al.; Int. J. Pharm.
495, 849 (2015),
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Identification and Immune Functional Characterization of Pigeon TLR7: D. Xiong, et al.; Int. J. Mol. Sci.
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Application(s): Injection into pigeons,
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Full Text
Adjuvant-carrying synthetic vaccine particles augment the immune response to encapsulated antigen and exhibit strong local immune activation without inducing systemic cytokine release: P.O. Ilyinskii, et al.; Vaccine
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B1 cells are unaffected by immune modulatory treatment in remitting-relapsing multiple sclerosis patients: D. Rovituso, et al.; J. Neuroimmunol.
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Monocytes from Chronic HBV Patients React In Vitro to HBsAg and TLR by Producing Cytokines Irrespective of Stage of Disease: A. Boltjes, et al.; PLoS One
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Myeloid-specific Rictor deletion induces M1 macrophage polarization and potentiates in vivo pro-inflammatory response to lipopolysaccharide: W.T. Festuccia, et al.; PLoS One
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Soluble CEACAM8 interacts with CEACAM1 inhibiting TLR2-triggered immune responses: B.B. Singer, et al.; PLoS One
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Cathepsin K is involved in development of psoriasis-like skin lesions through TLR-dependent Th17 activation: T. Hirai, et al.; J. Immunol.
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FANCA and FANCC modulate TLR and p38 MAPK-dependent expression of IL-1β in macrophages: M.R. Garbati, et al.; Blood
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Distinct TLR adjuvants differentially stimulate systemic and local innate immune responses in nonhuman primates: M. Kwissa, et al.; Blood
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Interleukin-15-induced CD56+ myeloid dendritic cells combine potent tumor antigen presentation with direct tumoricidal potential. : S. Anguille, et al.; PLoS One
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Immune response in the duck intestine following infection with low-pathogenic avian influenza viruses or stimulation with a Toll-like receptor 7 agonist administered orally: C. Volmer, et al.; J. Gen. Virol.
92, 534 (2011),
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The TLR7 agonist R848 alleviates allergic inflammation by targeting invariant NKT cells to produce IFN-gamma: F. Grela, et al.; J. Immunol.
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Abstract;
Treatment with the TLR7 agonist R848 induces regulatory T-cell-mediated suppression of established asthma symptoms: L. Pham Van, et al.; Eur. J. Immunol.
41, 1992 (2011),
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Differential induction of inflammatory cytokines by dendritic cells treated with novel TLR-agonist and cytokine based cocktails: targeting dendritic cells in autoimmunity: S.S. Jensen & M. Gad; J. Inflamm.
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Reciprocal regulation of activating and inhibitory Fc{gamma} receptors by TLR7/8 activation: implications for tumor immunotherapy: J.P. Butchar, et al.; Clin. Cancer Res.
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Systemic Toll-like receptor stimulation suppresses experimental allergic asthma and autoimmune diabetes in NOD mice: A. Aumeunier, et al.; PLOS ONE
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Toll-like receptor 7-triggered immune response in the lung mediates acute and long-lasting suppression of experimental asthma: C. Xirakia, et al.; Am. J. Respir. Crit. Care Med.
181, 1207 (2010),
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A novel polymorphism of the human CD40 receptor with enhanced function: A.L. Peters, et al.; Blood
112, 1863 (2008),
Abstract;
Treatment of intravaginal HSV-2 infection in mice: a comparison of CpG oligodeoxynucleotides and resiquimod (R-848): M.J. McCluskie, et al.; Antiviral Res.
69, 77 (2006),
Abstract;
Direct stimulation of human T cells via TLR5 and TLR7/8: flagellin and R-848 up-regulate proliferation and IFN-gamma production by memory CD4+ T cells: G. Caron, et al.; J. Immunol.
175, 1551 (2005),
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TLR agonists as vaccine adjuvants: comparison of CpG ODN and Resiquimod (R-848): R.D. Weeratna, et al.; Vaccine
23, 5263 (2005),
Abstract;
Resiquimod: a new immune response modifier with potential as a vaccine adjuvant for Th1 immune responses: J.J. Wu, et al.; Antiviral Res.
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Human TLR7 or TLR8 independently confer responsiveness to the antiviral compound R-848: M. Jurk, et al.; Nat. Immunol.
3, 499 (2002),
Abstract;
Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway: H. Hemmi, et al.; Nat. Immunol.
3, 196 (2002),
Abstract;
The immune response modifier resiquimod mimics CD40-induced B cell activation: G.A. Bishop, et al.; Cell. Immunol.
208, 9 (2001),
Abstract;
