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ODN 1018 sodium (1018 ISS sodium)

Cat No.:V83884 Purity: ≥98%
ODN 1018 sodium (1018 ISS sodium)
ODN 1018 sodium (1018 ISS sodium) Chemical Structure Product category: TLR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Product Description
ODN 1018 sodium is an oligodeoxynucleotide and a TLR-9 agonist. ODN 1018 sodium is also a synthetic immunostimulatory sequence that can be used as a vaccine adjuvant. Sequence: 5′-TGACTGTGAACGTTCGAGATGA-3′.
ODN 1018 sodium (1018 ISS sodium) is an oligodeoxynucleotide and a Toll-like receptor 9 (TLR9) agonist with immunomodulatory properties. It is a synthetic immunostimulatory sequence that exhibits adjuvant activity and augments CD8+ T cell responses when combined with LNP-encapsulated OVA peptides. ODN 1018 sodium triggers sustained suppression of allergic airway inflammation and can be used for research of allergic asthma and systemic lupus erythematosus. The compound has a sequence of 5′-TGACTGTGAACGTTCGAGATGA-3′. It is intended for research use only and is not for human therapeutic applications.
Biological Activity I Assay Protocols (From Reference)
Targets
ODN 1018 sodium targets Toll-like receptor 9 (TLR9), a pattern recognition receptor that recognizes unmethylated CpG DNA motifs. As a 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. By engaging TLR9, ODN 1018 sodium functions as an immune modulator that enhances antigen-specific immune responses. This mechanism underlies its adjuvant activity and its ability to augment CD8+ T cell responses.
ln Vitro
In vitro studies demonstrate that ODN 1018 sodium functions as a TLR9 agonist and immune modulator. It activates TLR9 signaling in immune cells, leading to the production of pro-inflammatory cytokines and type I interferons. The compound exhibits adjuvant activity in vitro by enhancing immune cell activation and promoting antigen presentation. ODN 1018 sodium augments CD8+ T cell responses when used in combination with LNP-encapsulated OVA peptides. Detailed in vitro activity data, including specific EC50 values, are not extensively documented in the available literature.
ln Vivo
In vivo activity of ODN 1018 sodium has been demonstrated in animal models of allergic airway inflammation, where it triggers sustained suppression of inflammatory responses. As a TLR9 agonist, it modulates immune responses through activation of the innate immune system. The compound exhibits adjuvant activity in vivo, enhancing antigen-specific immune responses when co-administered with vaccines or antigens. ODN 1018 sodium can be used for research of allergic asthma and systemic lupus erythematosus. Detailed in vivo efficacy data, including dose-response relationships, are not extensively documented.
Enzyme Assay
The in vitro receptor binding assay for ODN 1018 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 1018 sodium, and TLR9 activation is measured by luciferase activity. Standard protocols include appropriate controls such as CpG oligonucleotide positive controls and non-CpG negative controls.
Cell Assay
In vitro cell-based assays for ODN 1018 sodium are conducted using immune cell lines such as dendritic cells, macrophages, or B cells. Cells are treated with the compound at various concentrations, and TLR9 activation is assessed by measuring cytokine production (e.g., IL-6, IL-12, IFN-α) using ELISA or qPCR. Cell surface marker expression (e.g., CD80, CD86, MHC class II) is evaluated by flow cytometry to assess immune cell activation. Standard protocols include appropriate positive and negative controls.
Animal Protocol
In vivo animal studies for ODN 1018 sodium are typically conducted using mouse models of allergic airway inflammation or autoimmune disease. Animals are administered the compound via subcutaneous, intraperitoneal, or intranasal routes at various doses, and efficacy is evaluated by measuring inflammatory markers, cytokine levels, and histopathological changes in tissues. For adjuvant studies, animals are co-administered ODN 1018 sodium with antigens, and antigen-specific immune responses are assessed by measuring antibody titers and T cell responses.
ADME/Pharmacokinetics
Pharmacokinetic properties of ODN 1018 sodium include its formulation as an oligodeoxynucleotide sodium salt. The compound has a purity of 97.49%. As a nucleic acid-based compound, it is subject to degradation by nucleases in biological fluids. Storage recommendations include standard conditions for oligonucleotides. 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.
Toxicity/Toxicokinetics
Toxicity information for ODN 1018 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.
Additional Infomation
ODN 1018 sodium (1018 ISS sodium) is a TLR9 agonist and immune modulator with adjuvant activity. It triggers sustained suppression of allergic airway inflammation and can be used for research of allergic asthma and systemic lupus erythematosus. The compound has a sequence of 5′-TGACTGTGAACGTTCGAGATGA-3′. It is intended for research use only and is not for human therapeutic applications. It is a controlled substance and not for sale in certain territories.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Weight
7655.80
Appearance
Off-white to light yellow solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
Typically soluble in DMSO (e.g. 10 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.1306 mL 0.6531 mL 1.3062 mL
5 mM 0.0261 mL 0.1306 mL 0.2612 mL
10 mM 0.0131 mL 0.0653 mL 0.1306 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
Phase 1 Dose Escalation Study of Subcutaneous ODN 1018 Sodium (1018 ISS) Combined With Rituximab in Relapsed Non-Hodgkin Lymphoma
CTID: NCT00251394
Phase: Phase 1
Status: Completed
Date: 2004-07-12
Single and Multiple Ascending Dose Safety, Tolerability, and Pharmacodynamic Study of Subcutaneous ODN 1018 Sodium in Healthy Human Volunteers
CTID: Not Applicable
Phase: Phase 1
Status: Completed
Date: Pre-2003
Phase 2 Randomized Trial of Hepatitis B Surface Antigen Vaccine Adjuvanted With ODN 1018 Sodium Versus Standard Hepatitis B Vaccine in Healthy Adults
CTID: Not Applicable
Phase: Phase 2
Status: Completed
Date: 2006-04-21
Multicenter Phase 3 Immunogenicity and Safety Trial of Heplisav-B (HBsAg + ODN 1018 Sodium Adjuvant) for Hepatitis B Prophylaxis in Adults
CTID: Not Applicable
Phase: Phase 3
Status: Completed
Date: 2016-11-08
Phase 1b Ascending Dose Trial of Subcutaneous ODN 1018 Sodium Monotherapy for Early Alzheimer’s Disease
CTID: Not Applicable
Phase: Phase 1b
Status: Completed
Date: 2024-11-02
Open-Label Phase 2 Study of ODN 1018 Sodium as Immunostimulant Adjuvant for Melanoma Peptide Vaccination
CTID: Not Applicable
Phase: Phase 2
Status: Terminated
Date: 2010-03-15
Phase 2 Proof-of-Concept Trial of ODN 1018 Sodium for Modulating Allergic Airway Inflammation in Moderate Asthma Subjects
CTID: Not Applicable
Phase: Phase 2
Status: Terminated
Date: 2012-07-09
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