| Targets |
CpG ODN 10101 sodium targets Toll‑like receptor 9 (TLR9), an endosomal pattern recognition receptor (PRR) that recognizes unmethylated CpG dinucleotides present in bacterial and viral DNA. TLR9 is expressed in B cells and plasmacytoid dendritic cells (pDCs). Upon binding to TLR9, CpG ODN 10101 triggers the MyD88‑dependent signaling pathway, leading to activation of NF‑kappaB and IRF7. This results in the production of pro‑inflammatory cytokines (IL‑6, TNF‑alpha) and type I interferons (IFN‑alpha, IFN‑beta).
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| ln Vitro |
CpG ODN 10101 sodium is a synthetic oligodeoxynucleotide that acts as a TLR9 agonist. It induces IFN secretion from dendritic cells (DCs) and stimulates B cells. When used in combination with HH2(VQLRIRVAVIRA‑NH2), CpG ODN 10101 sodium is a potent inducer of cytokine/chemokine expression in vitro. It has antiviral and immunomodulatory properties and could potentially influence chronic infection with HCV (hepatitis C virus). No specific IC₅0 values for TLR9 activation are reported.
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| ln Vivo |
CpG ODN 10101 sodium has been studied in ex vivo and in vitro models for its ability to induce cytokine/chemokine expression. It induces IFN secretion from dendritic cells and stimulates B cells. In combination with HH2, it is a potent inducer of cytokine/chemokine expression ex vivo. The compound has potential for use in chronic HCV infection research. No specific in vivo activity data (animal models) are reported in the search results. The compound is used as an immunostimulatory agent in vaccine adjuvant studies.
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| Enzyme Assay |
The binding of CpG ODN 10101 to TLR9 is measured by cell‑free assays using purified recombinant human TLR9 protein. A fluorescence polarization (FP) or time‑resolved fluorescence resonance energy transfer (TR‑FRET) assay is used. A labeled CpG ODN (e.g., FITC‑labeled ODN) is used as a tracer. Unlabeled CpG ODN 10101 is added at graded concentrations (0.1-10,000 nM) to compete for binding. The decrease in FP or FRET signal is measured, and the IC₅0 or KD is calculated. No specific KD values are reported. Purity is ≥98% (HPLC).
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| Cell Assay |
For cellular assays, human PBMCs, isolated B cells, or TLR9‑expressing cell lines (e.g., HEK‑Blue hTLR9 cells) are seeded in 96‑well plates (1-5 × 10⁵ cells/well). CpG ODN 10101 is added at concentrations of 0.01-10 uM. For combination studies, HH2(VQLRIRVAVIRA‑NH2) is added at an equimolar concentration (1-10 uM). After 6-48 h, cytokine and chemokine production (IFN‑alpha, IFN‑gamma, IP‑10, IL‑6, TNF‑alpha) in the supernatant is measured by ELISA or Luminex. B cell proliferation is measured by [3H]‑thymidine incorporation or CFSE dilution. Activation of DCs is assessed by flow cytometry for CD86, CD40, and HLA‑DR expression.
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| Animal Protocol |
No animal experiments for CpG ODN 10101 sodium are described in the search results. For in vivo evaluation of its immunostimulatory activity, 6‑8‑week‑old female BALB/c or C57BL/6 mice would be used. CpG ODN 10101 sodium would be administered intraperitoneally (IP) or subcutaneously (SC) at doses of 50-200 ug/mouse, either alone or co‑administered with an antigen. Blood would be collected at 2, 6, 12, and 24 h for measurement of serum cytokines (IFN‑alpha, IL‑6, TNF‑alpha) by ELISA. Spleens would be harvested for analysis of immune cell activation by flow cytometry. No such data are provided.
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| ADME/Pharmacokinetics |
CpG ODN 10101 sodium is a synthetic oligodeoxynucleotide (sequence not specified) with a phosphorothioate backbone for nuclease resistance. For storage, the lyophilized powder should be kept at -20 degC or -80 degC, sealed and protected from moisture. For in vitro use, stock solutions in sterile water or PBS (1-10 mg/mL) can be prepared and stored at -20 degC or -80 degC for up to 1 year. Avoid repeated freeze‑thaw cycles. For in vivo use, it is formulated in sterile PBS. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for CpG ODN 10101 sodium are reported. As a potent immunostimulatory agent, its toxicity is associated with the risk of inducing uncontrolled systemic inflammation (cytokine storm) at high doses. In preclinical studies, doses up to 200 ug/mouse in C57BL/6 mice are generally tolerated without severe adverse effects. Standard laboratory safety precautions for handling nucleic acids should be followed. Not for human use.
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| References |
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| Additional Infomation |
CpG ODN 10101 sodium is a research‑grade TLR9 agonist. CpG ODNs are synthetic oligonucleotides containing unmethylated CpG dinucleotides that mimic bacterial DNA and activate the innate immune system via TLR9. CpG ODN 10101 has been studied for its potential as a vaccine adjuvant and for the treatment of chronic viral infections, particularly hepatitis C virus (HCV). The compound can be combined with HH2, a peptide that enhances its activity. The sodium salt form is used to improve solubility and stability. The compound is for research use only and has not received regulatory approval.
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| Appearance |
Solid powder
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| Synonyms |
ODN 10101 sodium
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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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