| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
MethADP triammonium targets the enzyme CD73 (ecto-5'-nucleotidase). This is a membrane-bound glycoprotein found on many cell types, including endothelial, immune, and cancer cells. It catalyzes the dephosphorylation of adenosine monophosphate (AMP) to adenosine, which is a key step in the production of extracellular adenosine, a potent immunosuppressive and anti-inflammatory molecule.
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| ln Vitro |
MethADP (20 and 100 μmol/L) inhibits the synthesis of adenosine in A498 cells triggered by 5'-AMP [1].
MethADP is a highly potent inhibitor of CD73. Its IC₅0 is in the low nanomolar range, though the exact value is not listed here. It is a competitive inhibitor that prevents the conversion of AMP to adenosine. In functional assays, MethADP triammonium (20 and 100 micromol/L) significantly inhibits 5'-AMP-induced adenosine formation in A498 human kidney epithelial cells. |
| ln Vivo |
Not available. The compound's activity as a CD73 inhibitor makes it useful for blocking adenosine production in vivo. This is relevant in oncology, where blocking CD73 with inhibitors like MethADP can relieve immunosuppression and enhance anti-tumor immune responses. Specific in vivo efficacy data is not provided.
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| Enzyme Assay |
Standard assays for CD73 activity are based on the release of inorganic phosphate. A protocol involves mixing a CD73 enzyme source (e.g., recombinant CD73 protein or plasma membrane preparations) with AMP and varying concentrations of MethADP triammonium in a suitable Tris-HCl buffer (pH 7.4). After incubation at 37degC, the amount of inorganic phosphate liberated from AMP is measured by a colorimetric method using malachite green reagent.
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| Cell Assay |
A standard cellular assay involves seeding CD73-expressing cells, such as A498 human kidney cells or various cancer cell lines, in a 96-well plate. After reaching confluency, the culture medium is replaced with a buffer containing AMP and MethADP triammonium. After a 30-60 minute incubation, the supernatant is collected. The concentration of adenosine produced is quantified by a standard HPLC-MS method or an enzyme-based adenosine assay kit. A decrease in adenosine concentration in the MethADP-treated group demonstrates CD73 inhibition.
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| Animal Protocol |
For in vivo studies, MethADP triammonium can be administered to tumor-bearing mouse models via intraperitoneal (IP) or intravenous (IV) injection. The typical dose might be 50-100 mg/kg. After treatment, blood or tumor tissue samples are analyzed for adenosine and AMP levels, and immune cell infiltration in the tumor is assessed by flow cytometry.
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| ADME/Pharmacokinetics |
MethADP triammonium is a stable and potent inhibitor. Its molecular weight is 476.32. It has a non-hydrolyzable methylene bridge between the alpha and beta phosphates, which makes it resistant to enzymatic degradation by phosphatases, a key feature for its use as a CD73 inhibitor. It is highly soluble in water (46.67 mg/mL, ~97.98 mM). For research use only; therapeutic use is not approved.
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| Toxicity/Toxicokinetics |
As an enzyme inhibitor, it is expected to be tolerated at effective doses. Potential toxicities would be related to the reversal of the immunosuppressive effects of adenosine, possibly leading to excessive inflammation or autoimmunity, but this is context-dependent and not inherent to the molecule itself.
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| References | |
| Additional Infomation |
MethADP triammonium is a research-grade, potent CD73 inhibitor. It is a crucial chemical tool for studying the roles of the CD73-adenosine pathway in cancer, inflammation, and ischemic injury. It is also used as a standard for in vitro assays. This product is strictly for laboratory research and is not intended for human therapeutic or diagnostic use. No CD73 inhibitor has yet received FDA approval for cancer therapy, though several are in clinical trials.
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| Molecular Formula |
C11H26N8O9P2
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| Molecular Weight |
476.32
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| Related CAS # |
MethADP;3768-14-7;MethADP sodium salt;89016-30-8
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| Appearance |
Off-white to light yellow 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~46.67 mg/mL (~97.98 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0994 mL | 10.4971 mL | 20.9943 mL | |
| 5 mM | 0.4199 mL | 2.0994 mL | 4.1989 mL | |
| 10 mM | 0.2099 mL | 1.0497 mL | 2.0994 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.
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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