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Resiquimod (R-848) (Synonyms: Resiquimod, S 28463)

Catalog No.GC13650

Resiquimod (R-848) is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.

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Resiquimod (R-848) Chemical Structure

Cas No.: 144875-48-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$59.00
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10mg
$54.00
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25 mg
$99.00
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50mg
$153.00
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100mg
$216.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Native mast cells

Preparation Method

The purified mast cells were incubated with medium alone or Resiquimod at a final concentration of 10 g/ml for 6 or 12 h at 37℃ in a humidified atmosphere with 5% CO2.

Reaction Conditions

10 µg/ml Resiquimod; 6 or 12 h

Applications

Resiquimod induced the increase of high-affinity IgE receptor (FcεRI) expression.

Animal experiment [2]:

Animal models

Female BALB/c mice

Preparation Method

Mice were inoculated subcutaneously with 4T1 cells. At day 6 after inoculation, mice were treated with vehicle (6% dimethyl sulfoxide + 94% normal saline) and Resiquimod [3 mg/kg, intraperitoneally (IP)] (n=5/group).

Dosage form

3 mg/kg Resiquimod;i.p ; three continuous days in a week for three weeks.

Applications

Resiquimod exhibits antitumoral effects in a murine breast cancer model.

References:

[1].Agier J, Brzezińska-Błaszczyk E,et,al.he impact of TLR7 agonist R848 treatment on mast cell phenotype and activity. Cell Immunol. 2021 Jan;359:104241. doi: 10.1016/j.cellimm.2020.104241. Epub 2020 Oct 28. PMID: 33158544.
[2].Yin T, He S,et,al. Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015 Sep;12(3):3515-3520. doi: 10.3892/mmr.2015.3885. Epub 2015 Jun 3. PMID: 26043701.

Background

Resiquimod (R848) is an imidazoquinoline compound with potential antiviral activity. It is a low molecular weight synthetic molecule that has been evaluated in clinical studies for the treatment of infections caused by viruses such as herpes simplex virus and hepatitis C virus[1]. Resiquimod was found to reduce viral shedding and viral reoccurrence by activating various immune cells to produce an environment conductive for the T-helper 1 (Th1) immune responses[2-3]. Resiquimod is a selective ligand for Toll-like receptor (TLR) 7 in mouse and for TLR7 and TLR8 in human and has been shown to activate only TLR7 and TLR8[4].

Resiquimod(10 µg/ml; 6 or 12 h) induced the increase of high-affinity IgE receptor (FcεRI) expression in native mast cells [5].

Resiquimod 8(3 mg/kg;i.p ; three continuous days in a week for three weeks) exhibited a robust antitumoral effect. Resiquimod reduced tumor vasculature and induced tumor cell apoptosis. Resiquimod increased high mobility group Box 1 expression in tumor tissues and activated CD4+ T cells in the peripheral blood[6]. Resiquimod (10 g; i.p) induces anti-tumor responses and attenuates cachexia in murine models of pancreatic ductal adenocarcinoma (PDAC)[7]. The combination of Resiquimod (3 mg/kg were administered by retro-orbital injections (diluted in PBS, 100 µL per mouse) 1 day before, 1 day after, and 1 week after SBRT treatments (total of 3 times))and SBRT results in significant immune activation of the pancreatic tumor microenvironment (TME), including increased tumor antigen-specific CD8+ T cells, decreased regulatory T cells, and enhanced antigen-presenting cells maturation, as well as increased interferon gamma, granzyme B, and CCL5 along with decreased levels of interleukin 4 (IL-4), IL-6, and IL-10[8].

References:
[1]. Miller RL, Meng TC,et,al. The antiviral activity of Toll-like receptor 7 and 7/8 agonists. Drug News Perspect. 2008 Mar;21(2):69-87. doi: 10.1358/dnp.2008.21.2.1188193. PMID: 18389099.
[2]. Bernstein DI, Harrison CJ, ,et,al. Daily or weekly therapy with resiquimod (R-848) reduces genital recurrences in herpes simplex virus-infected guinea pigs during and after treatment. J Infect Dis. 2001 Mar 15;183(6):844-9. doi: 10.1086/319262. Epub 2001 Feb 13. PMID: 11237799.
[3]. Wu JJ, Huang DB,et,al. Resiquimod: a new immune response modifier with potential as a vaccine adjuvant for Th1 immune responses. Antiviral Res. 2004 Nov;64(2):79-83. doi: 10.1016/j.antiviral.2004.07.002. PMID: 15498602.
[4]. Heil F, Hemmi H,et,al. Species-specific recognition of single-stranded RNA via toll-like receptor 7 and 8. Science. 2004 Mar 5;303(5663):1526-9. doi: 10.1126/science.1093620. Epub 2004 Feb 19. PMID: 14976262.
[5]. Agier J, Brzezińska-Błaszczyk E,et,al. The impact of TLR7 agonist R848 treatment on mast cell phenotype and activity. Cell Immunol. 2021 Jan;359:104241. doi: 10.1016/j.cellimm.2020.104241. Epub 2020 Oct 28. PMID: 33158544.
[6]. Yin T, He S,et,al.Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015 Sep;12(3):3515-3520. doi: 10.3892/mmr.2015.3885. Epub 2015 Jun 3. PMID: 26043701.
[7]. Michaelis KA, Norgard MA,et,al. The TLR7/8 agonist R848 remodels tumor and host responses to promote survival in pancreatic cancer. Nat Commun. 2019 Oct 15;10(1):4682. doi: 10.1038/s41467-019-12657-w. Erratum in: Nat Commun. 2019 Nov 15;10(1):5257. PMID: 31615993; PMCID: PMC6794326.
[8]. Ye J, Mills BN,et,al. Toll-like receptor 7/8 agonist R848 alters the immune tumor microenvironment and enhances SBRT-induced antitumor efficacy in murine models of pancreatic cancer. J Immunother Cancer. 2022 Jul;10(7):e004784. doi: 10.1136/jitc-2022-004784. PMID: 35851308; PMCID: PMC9295644.

Chemical Properties

Cas No. 144875-48-9 SDF
Synonyms Resiquimod, S 28463
Chemical Name 1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol
Canonical SMILES CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N
Formula C17H22N4O2 M.Wt 314.38
Solubility ≥ 33.8 mg/mL in EtOH with ultrasonic, ≥ 1.62 mg/mL in Water with ultrasonic and warming; 30 mg/mL in DMSO (Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1809 mL 15.9043 mL 31.8086 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL
10 mM 0.3181 mL 1.5904 mL 3.1809 mL
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