Highly pure and selective ligand for TLR7 and TLR8
Highly cited
R-848 is a selective ligand for Toll-like receptor 7 (TLR7) in mouse and for TLR7 and TLR8 in human. R-848 displays potent antitumor, proinflammatory, and anti-viral properties. R-848 stimulates antibody secretion, cytokine production (e.g. IL-6, IL-12, and IFNg), protection from apoptosis, and CD80 upregulation.
Product Details
Alternative Name:
4-Amino-2-(ethoxymethyl)-a,a-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol, S 28463, Resiquimod
Formula:
C17H22N4O2
MW:
314.4
Source:
Synthetic
CAS:
144875-48-9
Purity:
≥98% (HPLC)
Identity:
Identity determined by MS, 1H-NMR, and 13C-NMR.
Endotoxin Content:
Endotoxin-free
Appearance:
White to off-white solid.
Solubility:
Soluble in DMSO, 100% methanol, 5% methanol in dichloromethane; poorly soluble in acetonitrile or ethyl acetate.
Shipping:
Ambient Temperature
Long Term Storage:
-20°C
Regulatory Status:
RUO - Research Use Only
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Product Literature References
An Analysis of Linker-Dependent Effects on the APC Activation and In Vivo Immunogenicity of an R848-Conjugated Influenza Vaccine: K.F. Crofts, et al.; Vaccines 11, 1261 (2023), Abstract;
Blocking DCIR mitigates colitis and prevents colorectal tumors by enhancing the GM-CSF-STAT5 pathway: H. Sun, et al.; Cell Rep. 40, 111158 (2022), Abstract;
Drug-microenvironment perturbations reveal resistance mechanisms and prognostic subgroups in CLL: P.M. Bruch, et al.; Mol. Syst. Biol. 118, e10855 (2022), Abstract;
Drug‐microenvironment perturbations reveal resistance mechanisms and prognostic subgroups in CLL: P. Bruch, et al.; Mol. Syst. Biol. 18, e10855 (2022), Abstract; Full Text
Glycerol monolaurate inhibition of human B cell activation: M.G. Fosdick, et al.; Sci. Rep. 12, 13506 (2022), Abstract; Full Text
LL-37 as a Powerful Molecular Tool for Boosting the Performance of Ex Vivo-Produced Human Dendritic Cells for Cancer Immunotherapy: D. Stakheev, et al.; Pharmaceutics 14, 2747 (2022), Abstract;
RNPS1 inhibits excessive tumor necrosis factor/tumor necrosis factor receptor signaling to support hematopoiesis in mice: X. Zhong, et al.; PNAS 119, e2200128119 (2022), Abstract;
The mycotoxin Beauvericin exhibits immunostimulatory effects on dendritic cells via activating the TLR4 signaling pathway: X. Yang, et al.; Front. Immunol. 13, 856230 (2022), Abstract; Full Text
Endoplasmic reticulum stress sensor IRE1α propels neutrophil hyperactivity in lupus: S. Gautam, et al.; J. Clin. Invest. 131, e137866 (2021), Abstract;
Genetic and chemical inhibition of IRF5 suppresses pre-existing mouse lupus-like disease: T. Ban, et al.; Nat. Commun. 12, 4379 (2021), Abstract;
IRF-8/miR-451a regulates M-MDSC differentiation via the AMPK/mTOR signal pathway during lupus development: G. Shi, et al.; Cell Death Discov. 7, 41420 (2021), Abstract;
N4BP1 negatively regulates NF-κB by binding and inhibiting NEMO oligomerization: H. Shi, et al.; Nat. Commun. 12, 1379 (2021), Abstract;
Robust Antigen-Specific T Cell Activation within Injectable 3D Synthetic Nanovaccine Depots: J. Weiden, et al.; ACS Biomater. Sci. Eng. 7, 5622 (2021), Abstract;
Subversion of Lipopolysaccharide Signaling in Gingival Keratinocytes via MCPIP-1 Degradation as a Novel Pathogenic Strategy of Inflammophilic Pathobionts: A. Gasiorek, et al.; Mbio 12, 502 (2021), Abstract;
Terminal uridyltransferase 7 regulates TLR4-triggered inflammation by controlling Regnase-1 mRNA uridylation and degradation: C. Lin, et al.; Nat. Commun. 12, 3878 (2021), Abstract; Full Text
Thapsigargin-Stimulated LAD2 Human Mast Cell Line Is a Potent Cellular Adjuvant for the Maturation of Monocyte-Derived Dendritic Cells for Adoptive Cellular Immunotherapy: P. Taborska, et al.; Int. J. Mol. Sci. 22, 3978 (2021), Abstract; Full Text
The single-cell epigenomic and transcriptional landscape of immunity to influenza vaccination: F. Wimmers, et al.; Cell 184, 3915 (2021), Abstract; Full Text
TNF leads to mtDNA release and cGAS/STING-dependent interferon responses that support inflammatory arthritis: J. Willemsen, et al.; Cell Rep. 37, 109977 (2021), Abstract;
A Solid-in-Oil Nanodispersion System for Transcutaneous Immunotherapy of Cow's Milk Allergies: M. Kitaoka, et al.; Pharmaceutics 12, 205 (2020), Abstract;
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 12, 3766 (2020), Abstract; Full Text
Anti-neutrophil properties of natural gingerols in models of lupus: R.A. Ali, et al.; JCI Insight 2020, 138385 (2020), Abstract;
Inhibition of IRF5 cellular activity with cell-penetrating peptides that target homodimerization: J. Banga, et al.; Sci. Adv. 6, eaay1057 (2020), Abstract; Full Text
TLR7 in B cells promotes renal inflammation and Gd-IgA1 synthesis in IgA nephropathy: N. Zheng, et al.; JCI Insight 5, e136965 (2020), Abstract; Full Text
Urokinase-type plasminogen activator receptor is required for impairing toll-like receptor 7 signaling on macrophage efferocytosis in lupus: J. Li, et al.; Mol. Immunol. 127, 38 (2020), Abstract;
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 104, 392 (2019), Abstract; Full Text
The TLR7/8 agonist R848 remodels tumor and host responses to promote survival in pancreatic cancer: K.A. Michaelis, et al.; Nat. Commun. 10, 4682 (2019), Abstract; Full Text
Assessment of lung cell toxicity of various gasoline engine exhausts using a versatile in vitro exposure system: C. Bisig, et al.; Environ. Pollut. 235, 263 (2018), Abstract;
N-methyl-D-aspartate receptor antibody production from germinal center reactions: Therapeutic implications: M. Makuch, et al.; Ann. Neurol. 83, 553 (2018), Abstract; Full Text
Polymer-based nanoparticles loaded with a TLR7 ligand to target the lymph node for immunostimulation: J. Widmer, et al.; Int. J. Pharm. 535, 444 (2018), Abstract;
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. 91, e01844 (2017), Abstract;
Ligation of CD180 inhibits IFN-α signaling in a Lyn-PI3K-BTK-dependent manner in B cells: M. You, et al.; Cell. Mol. Immunol. 14, 192 (2017), Application(s): Cell culture, Abstract;
Activation of TLR7 increases CCND3 expression via the downregulation of miR-15b in B cells of systemic lupus erythematosus: D. Ren, et al.; Cell. Mol. Immunol. 13, 746 (2016), Application(s): Cell Culture, Abstract;
Ly6C+ monocyte efferocytosis and cross-presentation of cell-associated antigens: S.R. Larson, et al.; Cell Death Differ. 23, 997 (2016), Application(s): Efferocytosis assay, in vivo studies, Abstract; Full Text
NLRP3 activation and mitosis are mutually exclusive events coordinated by NEK7, a new inflammasome component: H. Shi, et al.; Nat. Immunol. 17, 250 (2016), Application(s): Stimulation of human monocytes, Abstract;
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. 7, e2341 (2016), Application(s): Ligand contribution to macrophage death in an autophagy-dependent way, Abstract; Full Text
Toll-like receptor 3 adjuvant in combination with virus-like particles elicit a humoral response against HIV: E. Poteet, et al.; Vaccine 34, 5886 (2016), Application(s): Cell culture for VesiVax CALV TLR formulations, Abstract;
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, Abstract; Full Text
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), Application(s): Cell Culture, Abstract;
Identification and Immune Functional Characterization of Pigeon TLR7: D. Xiong, et al.; Int. J. Mol. Sci. 16, 8364 (2015), Application(s): Injection into pigeons, Abstract; 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 32, 2882 (2014), Abstract;
B1 cells are unaffected by immune modulatory treatment in remitting-relapsing multiple sclerosis patients: D. Rovituso, et al.; J. Neuroimmunol. 272, 86 (2014), Abstract;
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 9, e97006 (2014), Abstract; Full Text
Myeloid-specific Rictor deletion induces M1 macrophage polarization and potentiates in vivo pro-inflammatory response to lipopolysaccharide: W.T. Festuccia, et al.; PLoS One 9, e95432 (2014), Abstract; Full Text
Soluble CEACAM8 interacts with CEACAM1 inhibiting TLR2-triggered immune responses: B.B. Singer, et al.; PLoS One 9, e94106 (2014), Abstract;
Cathepsin K is involved in development of psoriasis-like skin lesions through TLR-dependent Th17 activation: T. Hirai, et al.; J. Immunol. 190, 4805 (2013), Abstract;
FANCA and FANCC modulate TLR and p38 MAPK-dependent expression of IL-1β in macrophages: M.R. Garbati, et al.; Blood 122, 3197 (2013), Abstract;
Distinct TLR adjuvants differentially stimulate systemic and local innate immune responses in nonhuman primates: M. Kwissa, et al.; Blood 119, 2044 (2012), Abstract;
Interleukin-15-induced CD56+ myeloid dendritic cells combine potent tumor antigen presentation with direct tumoricidal potential. : S. Anguille, et al.; PLoS One 7, e51851 (2012), Application(s): Maturation of human dendritic cells, Abstract; Full Text
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), Abstract;
The TLR7 agonist R848 alleviates allergic inflammation by targeting invariant NKT cells to produce IFN-gamma: F. Grela, et al.; J. Immunol. 186, 284 (2011), 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), Abstract;
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. 7, 37 (2010), Abstract;
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. 16, 2065 (2010), Abstract; Full Text
Systemic Toll-like receptor stimulation suppresses experimental allergic asthma and autoimmune diabetes in NOD mice: A. Aumeunier, et al.; PLOS ONE 5, e11484 (2010), Abstract; Full Text
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), Abstract; Full Text
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), Abstract; Full Text
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. 64, 79 (2004), Abstract;
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;
