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| 10mg |
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Purity: ≥98%
Resiquimod (formerly known as R-848; S-28463; VML-600; R848, S27609) is a potent imidazoquinolinamine-based immune response modifier that acts as an agonist of the TLR 7/8 receptors (Toll-like receptor 7/8) with antiviral and antitumour activity. It can induce the levels of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod is the analogue of imiquimod (also called R-837,S-26308) with potential immunostimulatory activity. Resiquimod has been reported to dose-dependently induce cytokines including IFN, TNF, IL-1β and IL-6 in human peripheral blood mononuclear (PBMCs). In addition, Resiquimod has been revealed to stimulate intracellular IL-1β increased approximately 15%. The results have also been noted that both monocytes and B cells produced IFN in response to Resiquimod. On April 28, 2016, orphan designation (EU/3/16/1653) was granted by the European Commission to resiquimod for the treatment of cutaneous T-cell lymphoma.
| ln Vitro |
Resiquimod (R-848) causes circulating T cells (including TH2 effectors) that are specific to haptens and allergens to produce IFN-γ and even lose their capacity to produce IL-4 [2]. In BrdU incorporation experiments, resiquimod (R848) increases the number of BrdU-positive cells and, in a dose-dependent manner, boosts PBL proliferation. The reporter of NF-κB activity, luciferase, significantly increased (3.5-fold) in cells treated with R848 [3].
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| ln Vivo |
Rats and mice can be utilized as models for immune-mediated cardiac tissue injury and cytokine production with Resiquimod in animal modeling. In SPF chickens, the intramuscular injection of Resiquimod (R-848) at a dose of 50 μg/bird dramatically increased the production of IFN-α, IFN-β, IFN-γ, IL-1β, IL-4, iNOS, and MHC-II genes [1].
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| References |
[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 |
| Molecular Formula |
C17H22N4O2
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| Molecular Weight |
314.38
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| CAS # |
144875-48-9
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| Related CAS # |
Resiquimod-d5;2252319-44-9;Resiquimod;144875-48-9
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| SMILES |
CC(O)(C)CN1C(COCC)=NC2=C1C3=CC=CC=C3N=C2N
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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