| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Adenosine 5′-diphosphoribose sodium targets the TRPM2 channel. TRPM2 is a member of the transient receptor potential (TRP) family of ion channels. It is a non-selective cation channel that is permeable to Ca²⁺, Na⁺, and K⁺. TRPM2 is activated by ADP-ribose, which binds to the NUDT9 homology domain of the channel. Activation of TRPM2 leads to an influx of Ca²⁺ into the cell, which triggers various downstream signaling pathways. TRPM2 is involved in a wide range of physiological processes, including immune cell function, insulin secretion, neuronal cell death, and thermoregulation. Adenosine 5′-diphosphoribose is the most potent and primary activator of TRPM2. By activating TRPM2, Adenosine 5′-diphosphoribose sodium can modulate Ca²⁺ signaling and affect cellular functions. The compound also enhances autophagy, a cellular process involved in the degradation of damaged organelles and proteins.
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| ln Vitro |
Treatment with H2O2 activates poly(ADP-ribose) (PAR) polymerase-1 (PARP-1) in mouse embryonic stem cells (MEFs) to produce sodium adenosine 5′-bisphosphate ribose (ADP-ribose), a signal that activates the TRPM2 channel and promotes Ca2+ release via extracellular Ca2+ influx and/or lysosomes. In the end, this process determines whether to trigger early or late autophagy in response to various oxidations [1]. Adenosine 5'-ribose diphosphate (ADP-ribose) binds to the distinct intracellular NUDT9 homology (NUDT9-H) domain of TRPM2, which is found at its C terminator, to activate it. Intracellular Ca2+ is a significant co-activator alongside ADPR; the TRPM2 channel only opens in the presence of both ligands [2].
In vitro, Adenosine 5′-diphosphoribose sodium is used to activate TRPM2 channels in various cell types. It is the most potent and primary intracellular Ca²⁺-permeable cation TRPM2 channel activator. The compound's activity is typically assessed using patch-clamp electrophysiology or calcium imaging. In patch-clamp experiments, cells expressing TRPM2 are patch-clamped, and the compound is applied to the intracellular side of the membrane. The activation of TRPM2 is measured as an increase in current. In calcium imaging experiments, cells are loaded with a calcium-sensitive fluorescent dye, and the increase in intracellular calcium concentration upon application of the compound is measured. The compound also enhances autophagy, which can be measured by assessing the levels of autophagy markers, such as LC3-II, or by using fluorescent reporters. |
| ln Vivo |
Detailed in vivo activity data for Adenosine 5′-diphosphoribose sodium is limited. As a metabolite, it is produced intracellularly and is not typically administered exogenously in vivo. However, its role as a TRPM2 activator suggests that it plays a critical role in various physiological processes in vivo. For example, TRPM2 is involved in immune cell function, and ADP-ribose production is increased in response to oxidative stress. The compound's role in autophagy suggests that it may be involved in cellular stress responses. However, specific in vivo studies involving the administration of Adenosine 5′-diphosphoribose sodium are not detailed in the available literature. The compound is primarily used as a research tool for in vitro studies.
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| Enzyme Assay |
In a cell-free assay, the activation of TRPM2 by Adenosine 5′-diphosphoribose sodium is typically measured using patch-clamp electrophysiology or by using a fluorescent-based assay. In a patch-clamp experiment, TRPM2 channels are expressed in a heterologous system, such as HEK293 cells. Inside-out patches are excised, and varying concentrations of Adenosine 5′-diphosphoribose sodium are applied to the intracellular side of the membrane. The current through the TRPM2 channel is measured. The EC₅₀ for activation is determined from the dose-response curve. In a fluorescent-based assay, TRPM2 channels are expressed in cells, and the cells are loaded with a calcium-sensitive dye. The cells are then permeabilized to allow the compound to enter the cell, and the increase in fluorescence is measured. The EC₅₀ is determined from the dose-response curve. These assays provide a measure of the compound's ability to activate TRPM2.
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| Cell Assay |
For in vitro cellular assays, the effect of Adenosine 5′-diphosphoribose sodium on TRPM2 activation is typically assessed using cells expressing TRPM2, such as HEK293 cells transfected with TRPM2. Cells are loaded with a calcium-sensitive fluorescent dye, such as Fura-2 or Fluo-4. The cells are then treated with various concentrations of Adenosine 5′-diphosphoribose sodium, and the change in fluorescence is measured using a fluorescence microscope or a plate reader. The EC₅₀ for calcium influx is determined from the dose-response curve. The effect of the compound on autophagy is assessed by measuring the levels of LC3-II by Western blot or by using a fluorescent autophagy reporter. These assays provide a measure of the compound's activity in a cellular context.
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| Animal Protocol |
In vivo animal experiments involving Adenosine 5′-diphosphoribose sodium are not typical, as the compound is a charged molecule that does not readily cross cell membranes. However, studies may involve the use of inhibitors of ADP-ribose metabolism or the use of TRPM2 knockout mice to study the role of ADP-ribose and TRPM2 in vivo. For example, TRPM2 knockout mice can be used to study the role of TRPM2 in immune function, insulin secretion, or neuronal cell death. The effects of ADP-ribose on these processes can be inferred by comparing the phenotypes of wild-type and TRPM2 knockout mice. These studies provide indirect evidence for the in vivo role of ADP-ribose.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for Adenosine 5′-diphosphoribose sodium are not applicable in the traditional sense, as it is a charged metabolite that does not readily cross cell membranes. It is typically used as a tool for in vitro studies. When administered exogenously, the compound is unlikely to be absorbed or distributed due to its charged nature. The compound is soluble in water (50 mg/mL), which is important for its use in aqueous assays. Its metabolism involves hydrolysis by pyrophosphatases and other enzymes. The compound is not a drug and is not intended for therapeutic use.
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| Toxicity/Toxicokinetics |
Adenosine 5′-diphosphoribose sodium is generally considered to be non-toxic, as it is a natural metabolite. However, as a research chemical, standard safety precautions should be observed when handling this compound. No specific toxicity studies have been detailed in the public domain. The compound is not approved for clinical use.
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| References | |
| Additional Infomation |
Adenosine 5′-diphosphoribose sodium is a research tool for studying TRPM2 channels. It is a potent TRPM2 activator and enhances autophagy. It is not a drug.
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| Molecular Formula |
C₁₅H₂₂N₅NAO₁₄P₂
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| Molecular Weight |
581.30
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| Exact Mass |
581.054
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| CAS # |
68414-18-6
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| PubChem CID |
16218837
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
37
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| Complexity |
860
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LVIWKNSMPKNKBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H23N5O14P2.Na/c16-13-9-14(18-4-17-13)20(5-19-9)15-12(26)11(25)8(33-15)3-32-36(29,30)34-35(27,28)31-2-7(23)10(24)6(22)1-21;/h1,4-8,10-12,15,22-26H,2-3H2,(H,27,28)(H,29,30)(H2,16,17,18);
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| Synonyms |
Adenosine 5′diphosphoribose sodiumADP ribose sodium
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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 : ~125 mg/mL (~215.04 mM)
DMSO : ~25 mg/mL (~43.01 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (172.03 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7203 mL | 8.6014 mL | 17.2028 mL | |
| 5 mM | 0.3441 mL | 1.7203 mL | 3.4406 mL | |
| 10 mM | 0.1720 mL | 0.8601 mL | 1.7203 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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