| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Adenosine receptors (A1, A2A, A2B, A3), which are G-protein-coupled receptors. Unlabeled adenosine is an endogenous signaling molecule that regulates cardiovascular function, neuronal activity, immune responses, and sleep. Adenosine-d2 has the same receptor binding profile as unlabeled adenosine.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Adenosine-d2 has the same biological activity as unlabeled adenosine. Adenosine binds to A1 and A2A receptors with Ki values in the nanomolar range (e.g., A1 Ki ~310 nM). It induces vasodilation (via A2A), bradycardia (via A1), and inhibits platelet aggregation, neurotransmitter release, and inflammation. |
| ln Vivo |
Unlabeled adenosine has a very short half-life (seconds) and is used therapeutically for supraventricular tachycardia (6-12 mg IV) and as a pharmacological stress agent in myocardial perfusion imaging. Adenosine-d2 is not administered therapeutically but is used as a tracer in PK studies.
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| Enzyme Assay |
Membrane preparations from HEK293 cells expressing human A1 or A2A receptors (5-20 microg) are incubated with Adenosine-d2 (0.1-1000 nM) and a labeled antagonist (e.g., [3H]DPCPX for A1, 2 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 1 mM EDTA) at 25degC for 60 minutes. Nonspecific binding is determined with 10 microM unlabeled adenosine.
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| Cell Assay |
Adenosine-d2 is spiked into cell culture media (1-100 microM). Cells (e.g., cardiomyocytes, neurons, platelets) are treated, and downstream signaling (cAMP accumulation, Ca2+ flux) is measured. For analytical use, cells are lysed, and Adenosine-d2 is used as an internal standard for LC-MS/MS.
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| Animal Protocol |
Not applicable for internal standard. For tracer studies, Adenosine-d2 can be administered to rodents (e.g., 1-10 mg/kg IV), and blood and tissue samples are collected over 0-30 minutes for LC-MS/MS analysis to quantify adenosine metabolism and clearance rates.
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| ADME/Pharmacokinetics |
Adenosine has an extremely short plasma half-life (less than 10 seconds) due to rapid cellular uptake via equilibrative nucleoside transporters and rapid metabolism by adenosine deaminase. Adenosine-d2 behaves identically, enabling precise PK measurements via isotope dilution.
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| Toxicity/Toxicokinetics |
No toxicity; adenosine is an endogenous compound, and the d2-labeled version is safe at tracer levels. High therapeutic doses (140 microg/kg/min IV) can cause flushing, chest pain, bronchospasm, and transient heart block. The labeled version is used only at trace levels in research.
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| References |
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| Additional Infomation |
Adenosine-d2 is for research use only, not FDA-approved as a therapeutic. Unlabeled adenosine is FDA-approved for supraventricular tachycardia (Adenocard®) and for pharmacologic stress testing (Adenoscan®). The d2-labeled version is a valuable analytical internal standard for LC-MS/MS quantification of adenosine in biological fluids.
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| Molecular Formula |
C10H13N5O4
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|---|---|
| Molecular Weight |
267.241321325302
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| Exact Mass |
269.109
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| CAS # |
82741-17-1
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| Related CAS # |
Adenosine;58-61-7;Adenosine-15N5;168566-57-2
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| PubChem CID |
139025871
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| Appearance |
White to off-white solid powder
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| LogP |
-1.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
335
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1(O)[C@H]([n]2cnc3c(N)ncnc23)O[C@H](CO)C1O
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| InChi Key |
OIRDTQYFTABQOQ-QTYQXZHASA-N
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| InChi Code |
InChI=1S/C10H13N5O4/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(18)6(17)4(1-16)19-10/h2-4,6-7,10,16-18H,1H2,(H2,11,12,13)/t4-,6-,7-,10-/m1/s1/i1D2
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| Chemical Name |
(2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[dideuterio(hydroxy)methyl]oxolane-3,4-diol
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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) |
DMSO : ~125 mg/mL (~464.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7420 mL | 18.7098 mL | 37.4195 mL | |
| 5 mM | 0.7484 mL | 3.7420 mL | 7.4839 mL | |
| 10 mM | 0.3742 mL | 1.8710 mL | 3.7420 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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