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| Targets |
TLR3/7/9
ODN-2088 targets TLR3, TLR7, and TLR9. It acts as an inhibitor of these endosomal TLRs, preventing their activation by respective agonists (e.g., dsRNA for TLR3, ssRNA for TLR7, CpG DNA for TLR9). It blocks downstream MyD88-dependent and TRIF-dependent signaling pathways, reducing the release of pro-inflammatory cytokines. |
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| ln Vitro |
In human PBMC, ODN 2088 (0.01, 0.1, 1, 10 μM; 48 hours) does not cause cytotoxicity [1]. ODN 2088 (0.01, 0.1, 1, 10 μM; 24 h) blocks human PBMCs activated by TLR7-ligand RNA-ORN 22075 (5 μM) and CpG-ODN 2216 (3 μM) from releasing IFN-α[1]. Iripimod (5 μg/ml)-stimulated IL-6 release in human PBMC is inhibited by ODN 2088 (0.01, 0.1, 1, 10 μM; 48 h), although CpG-ODN 2006 (100 nM)-stimulated IL-6 release is weakly inhibited[1]. When B cells are activated with CpG-DNA 2006 (100 nM), ODN 2088 (0.1, 1, 10 μM; 24 h) hardly decreases IL-6 release; however, when humans are stimulated with imiquimod (5 μg/ml), IL-6 release from B cells is inhibited[1]. When CpG-ODN 2006 or imiquimod are not present, ODN 2088 (1, 10 μM; 48 hours) boosts the expression of CD86 and HLA-DR in CD20+ B cells [1]. ODN 2088 binds to the C-terminal region of TLR9 competitively, which may hinder CpG-ODN-induced TLR9-induced signaling [1]. When BMDM were treated with CpG-ODN 1826 (100 nM), ODN 2088 (0.001, 0.01, 0.1, 1, 10 μM; 24 h) demonstrated a dose-dependent suppression of TNF-α secretion, with a weekly inhibition. imiquimod, the agonist [3]. B cell proliferation is stimulated by ODN 2088 (10 μM) [3].
In human PBMCs, ODN-2088 (0.01-10 uM, 48 h) shows no cytotoxicity. It effectively inhibits the release of IFN-alpha and IL-6 induced by TLR3, TLR7, and TLR9 agonists, demonstrating its broad inhibitory activity against these key innate immune receptors. It is a useful tool for dissecting TLR signaling. |
| ln Vivo |
In vivo data are limited. ODN-2088 is a research tool for in vitro and ex vivo studies. It can be used to block TLR signaling in animal models to study the contribution of TLR3, TLR7, and TLR9 to inflammatory diseases, infections, and autoimmune conditions. Doses and routes of administration need to be optimized.
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| Enzyme Assay |
Not applicable. ODN-2088 is an oligonucleotide inhibitor that acts by competitively binding to TLR3, TLR7, and TLR9. Binding studies are typically performed in cell-based activation assays rather than cell-free systems. Standard protocols involve the use of purified TLR proteins and labeled ligands to measure displacement by ODN-2088.
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: human PBMC Tested Concentrations: 0.01, 0.1, 1, 10 μM Incubation Duration: 48 h Experimental Results: No cytotoxicity to human PBMC. Human PBMCs are isolated and seeded in 96-well plates. Cells are pre-incubated with ODN-2088 (0.01-10 uM) for 1-2 hours, then stimulated with specific TLR agonists (e.g., Poly(I:C) for TLR3, CL097 for TLR7, ODN-2006 for TLR9). After 18-24 hours, culture supernatants are collected for IFN-alpha and IL-6 measurement by ELISA. Cell viability is assessed by MTT. |
| Animal Protocol |
Tissue samples are collected from animals, and primary immune cells are isolated. Cells are pre-incubated with ODN-2088 (1-10 uM) for 1-2 hours, then stimulated with TLR agonists. For ex vivo analysis, animals are treated with a TLR agonist and ODN-2088. Blood and tissues (spleen, lymph nodes) are collected, and cytokine levels are measured.
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| ADME/Pharmacokinetics |
PK data are limited. ODN-2088 is soluble in H2O and formulated in endotoxin-free water or PBS. Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months. Molecular weight: 4878. Sequence: not provided in source. Purity: ≥98%.
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| Toxicity/Toxicokinetics |
Toxicity is minimal as ODN-2088 shows no cytotoxicity in human PBMCs up to 10 uM. Standard safety precautions for oligonucleotides apply. ODN-2088 is for research use only, not for human therapy. Avoid inhalation and contact. Use PPE in a well-ventilated area.
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| References |
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| Additional Infomation |
This is a research-grade TLR inhibitor. ODN-2088 is a specific antagonist of TLR3, TLR7, and TLR9 signaling. It is used as a negative control for CpG ODN studies and to investigate the role of TLRs in immune-mediated diseases. It does not inhibit TLR4 or TLR8. Purity: ≥98%.
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| CAS # |
1146541-45-8
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| Related CAS # |
Biotin-labeled ODN 2088 sodium;FITC-labeled ODN 2088 sodium
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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