1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)

Resiquimod (Synonyms: R848; S28463)

Cat. No.: HY-13740 Purity: 99.82%
Handling Instructions

Resiquimod 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.

For research use only. We do not sell to patients.

Resiquimod Chemical Structure

Resiquimod Chemical Structure

CAS No. : 144875-48-9

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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 204 In-stock
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100 mg USD 288 In-stock
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Customer Review

    Resiquimod purchased from MCE. Usage Cited in: Cytokine. 2017 Nov;99:310-315.

    IL-23 production by macrophages after stimulation with LPS or Resiquimod M1 macrophages (day 9) were stimulated with LPS (10 ng) or Resiquimod (5 μM) for 6 h and IL-23 protein is measured by ELISA.

    Resiquimod purchased from MCE. Usage Cited in: J Interferon Cytokine Res. 2016 Sep;36(9):563-72.

    With the stimulus of agonists LPS, ODN2006, Poly (I: C), and R848, the mRNA levels of goOASL in PBMCs are significantly upregulated (0.01
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Resiquimod 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.

    In Vitro

    Resiquimod (R-848) induces both hapten- and allergen-specific circulating T cells, including TH2 effectors, to produce IFN-γ and even to lose the ability to produce IL-4[2]. Resiquimod (R848) enhances PBL proliferation in a dose-dependent manner, and increases the number of BrdU-positive cells in BrdU incorporation assay. Cells treated with R848 exhibits significantly increased (3.5-fold) luciferase (a reporter of NF-κB activity) activity[3].

    In Vivo

    Resiquimod (R-848) (50 μg/bird, i.m. route) significantly up-regulates the expression of IFN-α, IFN-β, IFN-γ, IL-1β, IL-4, iNOS and MHC-II genes in SPF chicken[1].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (95.43 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    References
    Kinase Assay
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    For inhibition of lysosomal acidification, cells are incubated with 10 µM CQ for 1 h before Resiquimod (R848) treatment. After treatment, 20 µL of 5 mg/mL MTT is added to the plate. The plate is incubated at 22°C for 4 h, and 200 µL dimethyl sulfoxide is added to the plate to dissolve the reduced formazan. The plate is then read at 490 nm with a microplate reader. To determine the effect of Myd88 inhibition on R848-induced cell proliferation, the Myd88 inhibitor Pepinh-MYD and the control peptide Pepinh-Control are added to PBL at the concentration of 50 µM, and the plate is incubated at 22°C for 6 h. After incubation, the cells are treated with R848 and subjected to MTT assay as above. To determine the effect of NF-κB inactivation on R848-induced cell proliferation, BAY-11-7082, an irreversible inhibitor of IκB-α phosphorylation, is added to the cells at the concentration of 1 µM, and the plate is incubated at 22°C for 1 h. After incubation, the cells are treated with R848 and subjected to MTT assay as earlier. All experiments are performed three times.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    A total of 40 SPF chickens of two-week old are allotted to one of the following four experimental groups (n=10/group): Group A: PBS control; Group B: inactivated NDV vaccine; Group C: commercial oil adjuvanted inactivated NDV vaccine prepared from lentogenic strain and Group D: combination of inactivated NDV vaccine and R-848 (50 μg/bird). Vaccine or PBS is administered by intramuscular route in the thigh muscle. A booster dose is given 14-day post immunization (d.p.i). Two weeks post-booster, experimental SPF birds are challenged with velogenic strain of NDV (105 ELD50 per bird) intramuscularly. Clinical signs and mortality are observed daily till 14 day post-challenge (d.p.c). Cloacal swabs (n=6/group) are collected from the birds on day 0, 4, 7 and 14 post-challenge and inoculated into 10-day old embryonated chicken eggs (n=3 eggs/sample) through intra-allantoic route. Three day post-inoculation, the allantoic fluid is checked for the NDV growth by spot haemagglutination using 10% chicken RBC.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    314.38

    Formula

    C₁₇H₂₂N₄O₂

    CAS No.

    144875-48-9

    SMILES

    OC(C)(C)CN1C(COCC)=NC2=C1C3=CC=CC=C3N=C2N

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.82%

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    Product Name:
    Resiquimod
    Cat. No.:
    HY-13740
    Quantity:

    Resiquimod

    Cat. No.: HY-13740