| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
ODN TTAGGG targets three key DNA-sensing pathways in the innate immune system: Toll-like receptor 9 (TLR9), which recognizes unmethylated CpG DNA; the AIM2 inflammasome, which detects cytosolic DNA; and cGAS (cyclic GMP-AMP synthase), which also detects cytosolic DNA. It acts as an antagonist by competing with the natural ligands (CpG DNA or foreign DNA) for these receptors, thereby blocking their activation and the subsequent production of inflammatory cytokines.
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| ln Vitro |
In vitro, ODN TTAGGG potently inhibits the activation of TLR9, AIM2, and cGAS. In cell cultures, it prevents AIM2 inflammasome activation and cGAS activation by competing with DNA. This results in the suppression of pro-inflammatory cytokine secretion (e.g., IL-1beta, IL-6, TNF-alpha) from immune cells stimulated with DNA ligands. It is a valuable tool for studying the pathological role of these DNA sensors in autoimmune and inflammatory diseases.
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| ln Vivo |
In vivo, ODN TTAGGG has shown therapeutic potential in preclinical models of autoimmune diseases. Its immunosuppressive activity has been studied in models of lupus erythematosus, where it reduces the production of anti-DNA autoantibodies and kidney damage. By blocking TLR9 and AIM2, it alleviates the chronic inflammation and tissue damage associated with these disorders. It is being evaluated as a potential therapeutic for lupus and other autoinflammatory conditions.
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| Enzyme Assay |
For non-cell-based binding assays, a standard protocol uses a biotinylated CpG DNA ligand immobilized on a streptavidin-coated sensor chip. ODN TTAGGG is flowed over the chip at varying concentrations (0.1-10 microM). The binding affinity (KD) between ODN TTAGGG and recombinant human TLR9 extracellular domain is measured using Surface Plasmon Resonance (SPR). A direct competition assay can also be performed where ODN TTAGGG is premixed with CpG DNA before injection to measure inhibitory potency.
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| Cell Assay |
For in vitro cell assays, RAW 264.7 mouse macrophages are seeded in 96-well plates. Cells are treated with ODN TTAGGG at various concentrations (1-20 microM) for 1 hour. Then, a TLR9 agonist (e.g., ODN 1826, a CpG ODN) is added to the culture media. After 6 hours, supernatants are collected for cytokine measurement (e.g., TNF-alpha and IL-6) by ELISA. To measure AIM2 activation, human THP-1 macrophages are transfected with poly(dA:dT) (a synthetic DNA ligand) to activate AIM2. ODN TTAGGG is co-transfected to assess its inhibitory effect on IL-1beta secretion.
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| Animal Protocol |
For in vivo animal models, the lupus-prone MRL/lpr mouse model is used. Mice are administered ODN TTAGGG via intraperitoneal injection (e.g., 50-200 microg/mouse) three times per week for 8 weeks. Control mice receive a control ODN or PBS. Disease progression is monitored by measuring proteinuria (kidney damage) and anti-dsDNA antibody titers in serum. At study end, kidneys are harvested for histological assessment of glomerulonephritis, and spleens are analyzed for immune cell populations by flow cytometry.
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| ADME/Pharmacokinetics |
ODN TTAGGG is an oligonucleotide with a molecular weight of approximately 7944 Da. As a phosphorothioate-modified ODN (indicated by the "d(P-thio)" in the chemical name), it has enhanced resistance to nuclease degradation in serum, resulting in a longer in vivo half-life compared to unmodified DNA. This modification is critical for its in vivo efficacy. Standard PK would involve measuring plasma levels of intact ODN by HPLC or hybridization assays.
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| Toxicity/Toxicokinetics |
ODN TTAGGG is a research compound and not an approved drug. Toxicity studies in animals are required for its development as a therapeutic. Oligonucleotides of this class can sometimes be immunostimulatory rather than immunosuppressive at high doses. Their phosphorothioate backbone can also lead to non-specific protein binding and potential toxicities, such as transient complement activation or effects on coagulation time. This needs to be carefully characterized through pre-clinical safety studies.
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| References | |
| Additional Infomation |
ODN TTAGGG has potential for treating various autoimmune diseases, including systemic lupus erythematosus (SLE). The repetitive TTAGGG sequence is the telomeric repeat, and its mechanism of action is thought to mimic the immunosuppressive properties of mammalian telomeric DNA. It is also known as "A151" in the scientific literature. It is a valuable tool to dissect the relative contributions of TLR9, AIM2, and cGAS in inflammatory pathologies. It is not clinically approved and is for research use only.
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| Molecular Formula |
NA??MOLECULARWEIGHT
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| Molecular Weight |
0
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| CAS # |
1801724-76-4
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| Related CAS # |
Biotin-labeled ODN TTAGGG sodium;FITC-labeled ODN TTAGGG 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) |
H2O : ≥ 20 mg/mL (~2.52 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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