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.
With the stimulus of agonists LPS, ODN2006, Poly (I: C), and R848, the mRNA levels of goOASL in PBMCs are significantly upregulated in LPS- and Poly (I: C)-treated groups, and extremely upregulated in ODN2006- and R848-treated groups.
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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6
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.
IC50 & Target
TLR7
TLR8
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Resiquimod Related Antibodies
In Vivo
Resiquimod can be used to induce systemic lupus erythematosus models. Its pharmacokinetic characteristics feature a short half-life, a relatively low AUC at relevant doses, and a high Cmax[5].
Induction of systemic Lupus erythematosus[4].
Background
Alterations in TLR signaling contributes to the initiation and/or exacerbation of lupus in humans and in murine models. Autoreactive B cells (in which TLR-7 activation occurs in response to RNA-containing antigens), in synergy with B cell receptor, undergo proliferation, isotype switching, and plasma cell differentiation, leading to the production of autoantibodies.
Specific Mmodeling Methods
Mice: Wild-type FVB/N, BALB/c, and C57BL/6 mice • female • 7-9 weeks old (period: 4 weeks)
Administration: 100 μg • topical application to the right ear • three times a week for 4 weeks.
Note
(1) 100 μg of Resiquimod in 100 μL of Acetone.
Modeling Indicators
Metabolism changes: Elevates levels of autoantibodies to double-stranded DNA and multiple organ involvement, including glomerulonephritis, hepatitis, carditis. Histology analysis: Marked splenomegaly, and the liver revealed severe mononuclear cell infiltration around the portal veins and hepatocyte necrosis.
Correlated Product(s): Myosin H Chain Fragment, mouse (HY-P2464)
Opposite Product(s): Enpatoran (HY-134581)
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
Masse moléculaire
314.39
Formule
C17H22N4O2
CAS No.
144875-48-9
Appearance
Solid
Color
White to light yellow
SMILES
OC(C)(C)CN1C(COCC)=NC2=C1C3=CC=CC=C3N=C2N
Livraison
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvant et solubilité
In Vitro:
DMF : 50 mg/mL (159.04 mM; Need ultrasonic)
DMSO : ≥ 30 mg/mL (95.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Methanol : 25 mg/mL (79.52 mM; Need ultrasonic)
Ethanol : 25 mg/mL (79.52 mM; Need ultrasonic)
H2O : 0.1 mg/mL (0.32 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.1808 mL
15.9039 mL
31.8077 mL
5 mM
0.6362 mL
3.1808 mL
6.3615 mL
10 mM
0.3181 mL
1.5904 mL
3.1808 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Sachan S, et al. Adjuvant potential of resiquimod with inactivated Newcastle disease vaccine and its mechanism of action in chicken. Vaccine. 2015 Aug 26;33(36):4526-32.
[Content Brief]
[2]. Brugnolo F, et al. The novel synthetic immune response modifier R-848 (Resiquimod) shifts human allergen-specific CD4+ TH2 lymphocytes into IFN-gamma-producing cells. J Allergy Clin Immunol. 2003 Feb;111(2):380-8.
[Content Brief]
[3]. Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8-induced, Myd88- and NF-κB-dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113-20.
[Content Brief]
[4]. Maki Yokogawa, et al. Epicutaneous application of toll-like receptor 7 agonists leads to systemic autoimmunity in wild-type mice: a new model of systemic Lupus erythematosus. Arthritis Rheumatol. 2014 Mar;66(3):694-706.
[Content Brief]
[5]. Manuel Keppler, et al. Imidazoquinolines with improved pharmacokinetic properties induce a high IFNα to TNFα ratio in vitro and in vivo. Front Immunol. 2023 Jun 20:14:1168252.
[Content Brief]
Essai de kinase
[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Test cellulaire
[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale
[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références
[1]. Sachan S, et al. Adjuvant potential of resiquimod with inactivated Newcastle disease vaccine and its mechanism of action in chicken. Vaccine. 2015 Aug 26;33(36):4526-32.
[Content Brief]
[2]. Brugnolo F, et al. The novel synthetic immune response modifier R-848 (Resiquimod) shifts human allergen-specific CD4+ TH2 lymphocytes into IFN-gamma-producing cells. J Allergy Clin Immunol. 2003 Feb;111(2):380-8.
[Content Brief]
[3]. Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8-induced, Myd88- and NF-κB-dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113-20.
[Content Brief]
[4]. Maki Yokogawa, et al. Epicutaneous application of toll-like receptor 7 agonists leads to systemic autoimmunity in wild-type mice: a new model of systemic Lupus erythematosus. Arthritis Rheumatol. 2014 Mar;66(3):694-706.
[Content Brief]
[5]. Manuel Keppler, et al. Imidazoquinolines with improved pharmacokinetic properties induce a high IFNα to TNFα ratio in vitro and in vivo. Front Immunol. 2023 Jun 20:14:1168252.
[Content Brief]
[1]. Sachan S, et al. Adjuvant potential of resiquimod with inactivated Newcastle disease vaccine and its mechanism of action in chicken. Vaccine. 2015 Aug 26;33(36):4526-32.
[2]. Brugnolo F, et al. The novel synthetic immune response modifier R-848 (Resiquimod) shifts human allergen-specific CD4+ TH2 lymphocytes into IFN-gamma-producing cells. J Allergy Clin Immunol. 2003 Feb;111(2):380-8.
[3]. Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8-induced, Myd88- and NF-κB-dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113-20.
[4]. Maki Yokogawa, et al. Epicutaneous application of toll-like receptor 7 agonists leads to systemic autoimmunity in wild-type mice: a new model of systemic Lupus erythematosus. Arthritis Rheumatol. 2014 Mar;66(3):694-706.
[5]. Manuel Keppler, et al. Imidazoquinolines with improved pharmacokinetic properties induce a high IFNα to TNFα ratio in vitro and in vivo. Front Immunol. 2023 Jun 20:14:1168252.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
Methanol / Ethanol / DMSO / DMF
1 mM
3.1808 mL
15.9039 mL
31.8077 mL
79.5193 mL
5 mM
0.6362 mL
3.1808 mL
6.3615 mL
15.9039 mL
10 mM
0.3181 mL
1.5904 mL
3.1808 mL
7.9519 mL
15 mM
0.2121 mL
1.0603 mL
2.1205 mL
5.3013 mL
20 mM
0.1590 mL
0.7952 mL
1.5904 mL
3.9760 mL
25 mM
0.1272 mL
0.6362 mL
1.2723 mL
3.1808 mL
30 mM
0.1060 mL
0.5301 mL
1.0603 mL
2.6506 mL
40 mM
0.0795 mL
0.3976 mL
0.7952 mL
1.9880 mL
50 mM
0.0636 mL
0.3181 mL
0.6362 mL
1.5904 mL
60 mM
0.0530 mL
0.2651 mL
0.5301 mL
1.3253 mL
DMSO / DMF
80 mM
0.0398 mL
0.1988 mL
0.3976 mL
0.9940 mL
DMF
100 mM
0.0318 mL
0.1590 mL
0.3181 mL
0.7952 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Resiquimod Related Classifications
Inflammation/ImmunologyCancer
Cancer Targeted TherapyCancer Immunotherapy
Immunology/InflammationAnti-infection
Toll-like Receptor (TLR)HCV
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Resiquimod144875-48-9R848 S28463R 848R-848S28463S 28463S-28463Toll-like Receptor (TLR)HCVHepatitis C virusInhibitorinhibitorinhibit
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