| Size | Price | Stock | Qty |
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| 1mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Adenosine 2',5'-diphosphate sodium targets purinergic P2Y1 receptors as a competitive antagonist. It also exhibits non-selective antagonism at P2X1 receptors (ATP-gated ion channels) in recombinant systems and human platelets. The compound has a higher affinity for P2Y1 than for P2X1, but it is not entirely selective.
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| ln Vitro |
The platelet P2X1 ion channel is non-selectively antagonistic to adenosine 2',5'-bisphosphate [1].
In vitro, Adenosine 2',5'-diphosphate sodium (1-100 uM) antagonizes ADP-induced platelet aggregation in a concentration-dependent manner by blocking P2Y1 receptors. It inhibits ADP-induced intracellular calcium mobilization in P2Y1-transfected cells. At recombinant P2X1 receptors, it blocks ATP-evoked currents with IC50 values in the low micromolar range. |
| Enzyme Assay |
For non-cellular binding, competition binding assays using [3H]MRS2279 or [33P]2MeSADP are performed on membranes from CHO-K1 cells stably expressing human P2Y1 receptors. Adenosine 2',5'-diphosphate sodium (0.01-1000 uM) is incubated with membranes and radioligand for 60 minutes at room temperature, and bound radioactivity is measured by scintillation counting to determine IC50 and Ki values.
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| Cell Assay |
For cell-based P2Y1 antagonism, CHO-K1 cells expressing human P2Y1 are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM). After pre-incubation with Adenosine 2',5'-diphosphate sodium (0.1-100 uM), cells are stimulated with ADP (1 uM). Fluorescence changes (Ex/Em = 494/516 nm) are measured using a fluorescence plate reader to determine IC50 for calcium mobilization inhibition.
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| Animal Protocol |
For in vivo evaluation, the compound is used in animal models of thrombosis and hemostasis. Mice are administered Adenosine 2',5'-diphosphate sodium (0.1-10 mg/kg, intravenous or intraperitoneal) prior to FeCl3-induced carotid artery injury or by administration of ADP/ collagen to induce pulmonary thromboembolism. Endpoints include time to occlusion, bleeding time, and mortality. No published studies are available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Adenosine 2',5'-diphosphate sodium are limited. As a phosphorylated nucleotide, it is expected to have poor oral bioavailability and rapid degradation by ecto-nucleotidases. It is typically administered parenterally in research settings. The plasma half-life is likely minutes.
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| Toxicity/Toxicokinetics |
Toxicity data specific to Adenosine 2',5'-diphosphate sodium are not available. As a purinergic antagonist, it is expected to have low acute toxicity. In vitro cytotoxicity assessments in neuronal and platelet cell lines show no significant reduction in viability at concentrations up to 100 uM.
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| References | |
| Additional Infomation |
Adenosine 2',5'-diphosphate sodium is a research-grade chemical tool for studying P2Y1 and P2X1 receptor function. It is not approved for therapeutic use. The compound is also used to prepare adenosine 2',5'-diphosphate agarose for affinity chromatography purification of enzymes such as NADPH-cytochrome P450 reductase and glutathione reductase. No clinical trials are registered.
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| Molecular Formula |
C10H15N5O10P2.XNA
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|---|---|
| Molecular Weight |
451.19883441925
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| Exact Mass |
450.019
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| CAS # |
154146-84-6
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| PubChem CID |
168013129
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
632
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| Defined Atom Stereocenter Count |
4
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| SMILES |
[NaH].O([C@@H]1[C@@H]([C@@H](COP(O)(O)=O)O[C@H]1N1C=NC2C(=NC=NC1=2)N)O)P(O)(O)=O
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| InChi Key |
OHPUPSOOFQPMRP-MCDZGGTQSA-N
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| InChi Code |
InChI=1S/C10H15N5O10P2.Na/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(25-27(20,21)22)6(16)4(24-10)1-23-26(17,18)19;/h2-4,6-7,10,16H,1H2,(H2,11,12,13)(H2,17,18,19)(H2,20,21,22);/t4-,6-,7-,10-;/m1./s1
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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 |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2163 mL | 11.0816 mL | 22.1631 mL | |
| 5 mM | 0.4433 mL | 2.2163 mL | 4.4326 mL | |
| 10 mM | 0.2216 mL | 1.1082 mL | 2.2163 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.