Home Immunology & Inflammation TLR agonist Resiquimod (R-848)

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Resiquimod (R-848) TLR7/8 agonist

Cat.No.S8133

Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist, inducing the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. This compound reduces hepatitis C virus (HCV) infection. Phase 2.
Resiquimod (R-848) TLR agonist Chemical Structure

Chemical Structure

Molecular Weight: 314.38

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Quality Control

Batch: Purity: 99.98%
99.98

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC Function assay 30 nM 18 hrs Induction of type 1 IFN secretion in human PBMC at 30 nM after 18 hrs by ELISA, Activity=0.00125μM. 20232824
PBMC Function assay 10 nM 18 hrs Induction of type 1 IFN secretion in human PBMC at 10 nM after 18 hrs by ELISA, Activity<0.00125μM. 20232824
PBMC Function assay 100 nM 18 hrs Induction of type 1 IFN secretion in human PBMC at 100 nM after 18 hrs by ELISA, Activity=0.00561μM. 20232824
PBMC Function assay 300 nM 18 hrs Induction of type 1 IFN secretion in human PBMC at 300 nM after 18 hrs by ELISA, Activity=0.00726μM. 20232824
PBMC Function assay 1000 nM 18 hrs Induction of type 1 IFN secretion in human PBMC at 1000 nM after 18 hrs by ELISA, Activity=0.00775μM. 20232824
Huh7 Antiviral assay 48 hrs Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced mixed donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.024μM. 17548497
Huh7 Antiviral assay 48 hrs Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced single donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.0265μM. 17548497
PBMC Function assay 24 hrs Induction of IFNalpha2a level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=0.1μM. 17548497
PBMC Function assay 24 hrs Toxic induction of IL1-beta level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. 17548497
PBMC Function assay 24 hrs Toxic induction of IL6 level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. 17548497
PBMC Function assay 24 hrs Toxic induction of TNFalpha level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM. 17548497
HEK293 Function assay 6 hrs Agonist activity at human TLR7 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.1μM. 30143425
HEK293 Function assay Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601μM. 20232824
HEK293 Function assay 6 hrs Agonist activity at human TLR8 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.3μM. 30143425
HEK Function assay 8 to 12 hrs Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=1.34μM. 29152046
HEK Function assay 24 hrs Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=1.4μM. 22837811
HEK293 Function assay 24 hrs Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5μM. 24383475
HEK293 Function assay 6 hrs Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay, EC50=4μM. 27270029
HEK293 Function assay 24 hrs Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=4.5μM. 24383475
HEK Function assay 8 to 12 hrs Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=6.13μM. 29152046
HEK Function assay 24 hrs Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=6.4μM. 22837811
PBMC Function assay 24 hrs Increase in IFNalpha level in human PBMC after 24 hrs relative to control 17548497
PBMC Function assay 24 hrs Increase in 2',5'-oligoadenylate synthase level in human PBMC after 24 hrs relative to control 17548497
PBMC Toxicity assay 24 hrs Toxicity assessed as increase in IL6 level in human PBMC after 24 hrs relative to control 17548497
Huh7 Antiviral assay 24 hrs Antiviral activity against HCV infected human Huh7 replicon cells treated for 24 hrs with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay 17548497
Huh7 Antiviral assay Antiviral activity against HCV infected human Huh7 replicon cells treated with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay 17548497
PBMC Function assay 22.5 uM 24 hrs Agonist activity at TLR7/TLR8 in human PBMC assessed as induction of TNF-alpha production at 22.5 uM after 24 hrs by flow cytometric analysis 24383475
PBMC Immunomodulatory assay 16 uM 24 hrs Immunomodulatory activity in human PBMC assessed as induction of IL-6 secretion at 16 uM after 24 hrs by ELISA 28254484
BMD Function assay 1 uM 48 hrs Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD86 at 1 uM after 48 hrs by flow cytometry 19299126
BMD Function assay 1 uM 48 hrs Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of MHC class-2 at 1 uM after 48 hrs by flow cytometry 19299126
BMD Function assay 1 uM 48 hrs Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD40 at 1 uM after 48 hrs by flow cytometry 19299126
BMD Function assay 5 uM 24 hrs Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as IL12 production at 5 uM after 24 hrs by ELISA 19299126
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (197.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 51 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 314.38 Formula

C17H22N4O2

 Storage (From the date of receipt)
CAS No. 144875-48-9 Download SDF Storage of Stock Solutions

Synonyms S28463 Smiles CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N

Mechanism of Action

Targets/IC50/Ki
TLR7
TLR8
In vitro

Resiquimod (R-848) activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway.

This compound also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses.

It induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs.

In vivo

In wild-type mice, Resiquimod (R-848) (50 nmol, i.p.) induces increased serum concentrations of IFN-alpha, TNF-alpha and IL-12, while neither TLR7-deficient mice nor MyD88-deficient mice show an increase in these cytokines.

In a murine model of allergic asthma, this compound (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/26851512/
  • [5] https://pubmed.ncbi.nlm.nih.gov/25475963/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06021002 Recruiting
Innate Inflammatory Response|Asthma|Nasal Allergy
Cambridge University Hospitals NHS Foundation Trust
 August 9 2022 Not Applicable
NCT04127864 Active not recruiting
Colorectal Cancer|Surgery
University of Copenhagen|Zealand University Hospital
 October 14 2019 --
NCT02688478 Unknown status
Allergies
University of British Columbia
 February 2 2017 Not Applicable
NCT00960752 Completed
Melanoma
M.D. Anderson Cancer Center
 May 20 2010 Phase 2

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