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

Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.

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Resiquimod

Resiquimod Chemische Struktur

CAS. Nr. : 144875-48-9

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Beschreibung

Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages[1][2][3].

IC50 & Target[1]

TLR7

 

TLR8

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.75 3
Compound: R848
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
1.5 3
Compound: 2
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
1.4 3
Compound: 2
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
HEK293 EC50
0.75 3
Compound: R848
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
1.4 3
Compound: 2
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
HEK293 EC50
1.5 3
Compound: 2
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
4.5 3
Compound: 2
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
260.1 1
Compound: 2
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
[PMID: 20232824]
HEK293 EC50
4 3
Compound: Resiquimod
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
[PMID: 27270029]
HEK293 EC50
5.87 3
Compound: R848
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
4.5 3
Compound: 2
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
4 3
Compound: Resiquimod
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
[PMID: 27270029]
HEK293 EC50
5.87 3
Compound: R848
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
6.4 3
Compound: 2
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
HEK293 EC50
0.75 3
Compound: R848
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
6.4 3
Compound: 2
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
PBMC EC50
24 1
Compound: R848
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
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
[PMID: 17548497]
HEK293 EC50
1.4 3
Compound: 2
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
PBMC EC50
24 1
Compound: R848
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
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
[PMID: 17548497]
PBMC EC50
26.5 1
Compound: R848
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
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
[PMID: 17548497]
HEK293 EC50
1.5 3
Compound: 2
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
260.1 1
Compound: 2
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
[PMID: 20232824]
PBMC EC50
26.5 1
Compound: R848
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
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
[PMID: 17548497]
HEK293 EC50
260.1 1
Compound: 2
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
[PMID: 20232824]
HEK293 EC50
4 3
Compound: Resiquimod
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay
[PMID: 27270029]
HEK293 EC50
4.5 3
Compound: 2
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay
[PMID: 24383475]
HEK293 EC50
5.87 3
Compound: R848
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay
[PMID: 32001135]
HEK293 EC50
6.4 3
Compound: 2
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay
[PMID: 22837811]
PBMC EC50
24 1
Compound: R848
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
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
[PMID: 17548497]
PBMC EC50
26.5 1
Compound: R848
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
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
[PMID: 17548497]
In Vitro

Resiquimod (GMP) (3 µg/mL, 5 days) induces human mMDSC to mature into inflammatory macrophage (MACinflam)[1].
Resiquimod (GMP) (3 µg/mL, 3 days) produces IL-6 and IL-12 in human mMDSC[1].
Resiquimod (GMP) (2.5 µg/mL, 7 days) transdifferentiaes memory B cells to IgG producing plasma cells[2].
Resiquimod (GMP) (5 µg/mL, 5 days) induces the differentiation of MDSCs into mature myeloid cells[3].

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

Molekulargewicht

314.38

Formel

C17H22N4O2

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation
Verweise
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