Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Resiquimod [144875-48-9]

Imprimer

Référence HY-13740-50mg

Conditionnement : 50mg

Marque : MedChemExpress

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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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.75 μM 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 μM 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 μM 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 nM 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 μM 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 μM 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 μM 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 μM 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 nM 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 nM 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 (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.

In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

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 C_max^[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 Modeling 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:

DMSO : 100 mg/mL (318.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 50 mg/mL (159.04 mM; Need ultrasonic)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1808 mL	15.9038 mL	31.8076 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.

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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)
Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.95%

Fiche technique (290 KB) SDS (634 KB)

COA (254 KB) HNMR (201 KB) LCMS (119 KB)

Instruction de manipulation (2659 KB)

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]

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Référence HY-13740-50mg

Marque : MedChemExpress

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