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| 1mg |
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| Other Sizes |
| Targets |
ODN 2216 sodium targets Toll-like receptor 9 (TLR9), a pattern recognition receptor that recognizes unmethylated CpG DNA motifs. As a human-specific TLR9 agonist, it activates the innate immune system through the MyD88-dependent signaling pathway, leading to the production of pro-inflammatory cytokines and type I interferons. The compound induces significant production of IFN-α and IFN-β, and stimulates IFN-α through pDC (plasmacytoid dendritic cells) and IL-12(p40) through DC (dendritic cells).
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| ln Vitro |
In vitro studies demonstrate that ODN 2216 sodium is a human-specific TLR9 agonist that induces significant production of IFN-α and IFN-β. It stimulates IFN-α through pDC (plasmacytoid dendritic cells) and produces IL-12(p40) via DC (dendritic cells). ODN 2216 triggers peripheral blood mononuclear cells (PBMC) to produce IFN-γ indirectly, mediated by IFN-α/β. Additionally, ODN 2216 sodium can activate NK cells and enhance IFN-γ production in TCR-triggered CD4+ T cells.
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| ln Vivo |
In vivo activity of ODN 2216 sodium is related to its function as a TLR9 agonist that modulates immune responses through activation of the innate immune system. By inducing IFN-α, IFN-β, and IL-12(p40), the compound promotes Th1-type immune responses and enhances antigen-specific immunity. It can activate NK cells and enhance IFN-γ production in TCR-triggered CD4+ T cells. The compound is used to study TLR9-mediated immune activation and its role in vaccine adjuvants and immunotherapies.
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| Enzyme Assay |
The in vitro receptor binding assay for ODN 2216 sodium typically involves measuring its agonistic activity at Toll-like receptor 9 (TLR9). Cell-based reporter assays using HEK293 cells expressing human TLR9 and an NF-κB-driven luciferase reporter are commonly employed. Cells are treated with varying concentrations of ODN 2216 sodium, and TLR9 activation is measured by luciferase activity. Cytokine production (IFN-α, IFN-β, IL-12) is measured by ELISA in pDC or DC cultures. Standard protocols include appropriate controls such as CpG oligonucleotide positive controls and non-CpG negative controls.
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| Cell Assay |
In vitro cell-based assays for ODN 2216 sodium are conducted using human pDC (plasmacytoid dendritic cells) and DC (dendritic cells) cultures. Cells are treated with the compound at various concentrations, and TLR9 activation is assessed by measuring cytokine production (IFN-α, IFN-β, IL-12) using ELISA or qPCR. Cell surface marker expression is evaluated by flow cytometry to assess immune cell activation. PBMC cultures are used to measure IFN-γ production. NK cell activation and IFN-γ production in TCR-triggered CD4+ T cells are also evaluated.
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| Animal Protocol |
In vivo animal studies for ODN 2216 sodium are typically conducted using mouse models to evaluate TLR9-mediated immune activation. Animals are administered the compound via subcutaneous, intraperitoneal, or intranasal routes at various doses. Immune responses are assessed by measuring serum cytokine levels (IFN-α, IFN-β, IL-12, IFN-γ), NK cell activation, and T cell responses. The compound's adjuvant activity and its ability to enhance antigen-specific immune responses are evaluated in vaccine models. Standard protocols include appropriate controls such as vehicle-treated groups and known TLR9 agonists.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ODN 2216 sodium include its appearance as a white to off-white solid with 97.88% purity. Storage recommendations include lyophilized powder at -20 to -80°C for 1 year. As a nucleic acid-based compound, it is subject to degradation by nucleases in biological fluids. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not extensively documented in the available literature. The compound is intended for research use only and is not for human therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicity information for ODN 2216 sodium is limited in the available literature. As a TLR9 agonist, it may induce inflammatory responses that could lead to dose-dependent toxicity. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed acute or chronic toxicity data are available from the search results. The compound is a controlled substance and not for sale in certain territories.
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| Additional Infomation |
ODN 2216 sodium is a human-specific TLR9 ligand or agonist that induces significant production of IFN-α and IFN-β. It stimulates IFN-α through pDC and produces IL-12(p40) via DC. ODN 2216 triggers PBMC to produce IFN-γ indirectly and can activate NK cells and enhance IFN-γ production in TCR-triggered CD4+ T cells. It appears as a white to off-white solid with 97.88% purity. It is intended for research use only.
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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) |
Typically soluble in DMSO (e.g. 10 mM)
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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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