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| Targets |
TLR7/8 agonist 3 targets Toll-like receptors 7 and 8 (TLR7 and TLR8), which are pattern recognition receptors of the innate immune system. TLR7 and TLR8 recognize single-stranded RNA (ssRNA) and are involved in the detection of viral infections and the activation of immune responses. Upon activation, TLR7 and TLR8 initiate signaling cascades that lead to the production of type I interferons and pro-inflammatory cytokines, which are essential for antiviral immunity and immune modulation. TLR7/8 agonist 3 is a potent dual agonist that activates both TLR7 and TLR8. Its imidazoquinoline structure is characteristic of TLR7/8 agonists. The compound's dual activity makes it a valuable tool for immunology, vaccine adjuvant research, and cancer immunotherapy development.
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| ln Vitro |
In vitro, TLR7/8 agonist 3 demonstrates anti-leishmanial activity with an IC₅₀ of 5.93 µM against intracellular amastigotes. The compound is a potent dual agonist of TLR7 and TLR8. Activation of TLR7 and TLR8 leads to the production of type I interferons and pro-inflammatory cytokines, which are essential for antiviral immunity and immune modulation. The compound's dual TLR7/8 activity makes it a valuable tool for studying innate immune signaling, immune modulation, and therapeutic strategies targeting infectious disease and oncology. TLR7/8 agonist 3 provides a versatile probe for both in vitro and in vivo applications. The compound's activity is concentration-dependent, with efficacy observed in the low micromolar range.
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| ln Vivo |
In vivo, TLR7/8 agonist 3 is a valuable tool for vaccine adjuvant research and cancer immunotherapy development. Activation of TLR7 and TLR8 enhances immune responses, making the compound a potential adjuvant for vaccines. In cancer immunotherapy, TLR agonists can stimulate anti-tumor immune responses by activating dendritic cells, natural killer cells, and other immune cells. The compound's anti-leishmanial activity suggests potential applications in infectious disease therapy. However, detailed in vivo efficacy, pharmacokinetic, and toxicological data for TLR7/8 agonist 3 require further investigation from primary research publications. The compound is supplied as a research chemical for immunology research.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cellular) assays for TLR7/8 agonist 3 involve measuring binding affinity to TLR7 and TLR8 using surface plasmon resonance (SPR) or other biophysical methods. In these assays, recombinant TLR7 or TLR8 proteins are immobilized on a sensor chip, and varying concentrations of the compound are flowed over the chip. The binding response is measured in real-time, and the dissociation constant (Kd) is calculated from the binding curves. Alternatively, cell-based reporter assays may be used to assess TLR7/8 activation. In these assays, cells expressing TLR7 or TLR8 and a reporter gene (e.g., NF-κB-driven luciferase) are treated with the compound, and reporter activity is measured. These assays help characterize the compound's potency and selectivity for TLR7 and TLR8.
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| Cell Assay |
In vitro cellular experiments with TLR7/8 agonist 3 are performed using immune cells such as peripheral blood mononuclear cells (PBMCs), dendritic cells, or reporter cell lines expressing TLR7 or TLR8. Cells are cultured in appropriate media and treated with varying concentrations of the compound for 24-72 hours. TLR7/8 activation is assessed by measuring the production of cytokines (e.g., IFN-α, TNF-α, IL-6, IL-12) using ELISA or multiplex assays. Cell surface marker expression (e.g., CD80, CD86, HLA-DR) is assessed by flow cytometry to evaluate dendritic cell maturation. For anti-leishmanial activity, intracellular amastigotes are cultured in macrophages, and parasite burden is assessed by microscopy or by measuring parasite viability using fluorescent dyes. The compound's IC₅₀ of 5.93 µM against intracellular amastigotes is determined in these assays.
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| Animal Protocol |
In vivo animal studies with TLR7/8 agonist 3 have not been extensively reported. For vaccine adjuvant studies, mice are immunized with antigen and TLR7/8 agonist 3, and immune responses are assessed by measuring antibody titers, cytokine production, and T cell responses. For cancer immunotherapy studies, tumor-bearing mice are treated with the compound, and tumor growth inhibition and survival rates are assessed. For infectious disease studies, animal models of leishmaniasis or viral infection may be used to assess the compound's efficacy. The compound's dual TLR7/8 activity makes it a promising candidate for various immunotherapy applications.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TLR7/8 agonist 3 are not extensively characterized. The compound has molecular formula C₁₇H₂₃N₅O and molecular weight 313.4. As a small molecule (molecular weight 313.4), it is expected to have reasonable oral bioavailability and tissue distribution. The compound is a synthetic imidazoquinoline derivative, a class known for good oral bioavailability. Storage: -80°C. Detailed pharmacokinetic parameters including half-life, clearance, and bioavailability require further investigation from primary research publications.
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| Toxicity/Toxicokinetics |
Toxicological information for TLR7/8 agonist 3 is not extensively detailed in the available literature. As a research compound with immune-stimulatory activity, it should be handled with appropriate safety precautions. Standard safety guidelines for handling potent pharmaceutical compounds apply, including use of personal protective equipment (gloves, safety goggles, lab coat), working in a well-ventilated area, and proper chemical waste disposal. The compound is intended for research use only and is not approved for human therapeutic use. Cytotoxicity studies in cell-based assays help establish the therapeutic window and selectivity index of the compound.
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| References | |
| Additional Infomation |
TLR7/8 agonist 3 (CAS 642473-95-8) is a potent dual agonist of Toll-like receptors 7 and 8 (TLR7 and TLR8). The compound has molecular formula C₁₇H₂₃N₅O and molecular weight 313.4. TLR7/8 agonist 3 is a synthetic small-molecule imidazoquinoline derivative disclosed in patent WO2016057618, compound of formula (II). The compound demonstrates anti-leishmanial activity with an IC₅₀ of 5.93 µM against intracellular amastigotes. With its dual TLR7/8 activity, this compound is a valuable tool for immunology, vaccine adjuvant research, and cancer immunotherapy development. Storage: -80°C.
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| Molecular Formula |
C17H23N5O
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| Molecular Weight |
313.3974
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| Exact Mass |
313.19
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| CAS # |
642473-95-8
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| PubChem CID |
10380870
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| Appearance |
White to off-white solid powder
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| LogP |
3.722
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
404
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOCC1=NC2=C(N1CC(C)(C)N)C3=CC=CC=C3N=C2N
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| InChi Key |
SVBZCXQPNPURIX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H23N5O/c1-4-23-9-13-21-14-15(22(13)10-17(2,3)19)11-7-5-6-8-12(11)20-16(14)18/h5-8H,4,9-10,19H2,1-3H3,(H2,18,20)
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| Chemical Name |
1-(2-amino-2-methylpropyl)-2-(ethoxymethyl)imidazo[4,5-c]quinolin-4-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~50 mg/mL (~159.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.98 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.98 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL | |
| 5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL | |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1908 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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