| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Human Endogenous Metabolite
Diadenosine pentaphosphate pentaammonium acts through various purinergic receptors (P2X and P2Y subtypes) in the nervous system. It is a ligand for P2 purinergic receptors, with selectivity for certain receptor subunits. Additionally, it activates 5′-nucleotidase, an enzyme involved in nucleotide metabolism, and inhibits adenosine kinase activity, thereby modulating extracellular adenosine levels. Its effects are mediated through multiple receptor subtypes depending on the target tissue. |
|---|---|
| ln Vitro |
In vitro, diadenosine pentaphosphate pentaammonium activates 5′-nucleotidase and inhibits adenosine kinase. It induces calcium ion ([Ca2+]i) increases in rat basal ganglia aminergic terminals. The compound is metabolized by soluble enzymes in blood plasma and by membrane-bound ectoenzymes on endothelial and smooth muscle cells. It also stimulates gluconeogenesis in isolated rat proximal tubules and interacts with specific receptors in insulin-secreting cells.
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| ln Vivo |
In vivo studies have shown that diadenosine pentaphosphate pentaammonium affects biological activities in a wide range of target tissues. It acts as a signaling molecule in the heart and influences diadenosine polyphosphate-stimulated gluconeogenesis in rat proximal tubules. The compound is released into the extracellular space from secretory granules and is rapidly metabolized. It also modulates endogenous adenosine levels in rat brain by inhibiting adenosine kinase activity.
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| Enzyme Assay |
For non-cellular assays, a typical experimental setup involves a FRET (Förster resonance energy transfer) assay using an 11-amino acid peptide substrate to measure proteasome activity. The compound is incubated with purified 20S proteasome and the substrate, and fluorescence is measured. Alternatively, enzyme inhibition assays for AChE and BuChE are conducted using Ellman's method, where the compound is added to the enzyme and substrate, and the production of thiocholine is monitored spectrophotometrically at 405 nm. For 5′-nucleotidase activation, the enzyme is incubated with AMP and the compound, and the release of inorganic phosphate is quantified.
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| Cell Assay |
For cell-based assays, cells (e.g., chromaffin cells, neuronal cells, or hepatocytes) are cultured in appropriate media and treated with varying concentrations of Ap5A (0.1-100 microM) for 1-24 hours. Cellular responses such as calcium flux (using Fluo-4 AM dye), gluconeogenesis (measuring glucose production), or ATP levels (via luciferase assay) are assessed. For toxicity studies, cell viability is measured using MTT or CellTiter-Glo assays after 24-72 hour exposure. Negative controls (vehicle only) and positive controls (known agonists) should be included.
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| Animal Protocol |
In vivo experimental protocols typically use rodent models (rats or mice). The compound is administered intravenously (IV) or intraperitoneally (IP) at doses ranging from 0.1-10 mg/kg. Blood samples are collected at multiple time points to measure plasma concentrations and metabolism. Tissue distribution can be assessed by harvesting organs (brain, heart, liver) post-administration. For functional studies, parameters such as blood pressure, heart rate, or glucose levels are monitored. Ap5A is metabolized by soluble enzymes in blood plasma and membrane-bound ectoenzymes, with a short half-life in circulation. The compound is prepared in water or saline and stored at -20degC.
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| ADME/Pharmacokinetics |
As an endogenous metabolite, diadenosine pentaphosphate pentaammonium is naturally occurring and generally considered to have low toxicity at physiological concentrations. No significant acute toxicity has been reported in standard assays. In cell-based assays, it exhibits minimal cytotoxicity at concentrations up to 100 microM in most cell types. However, as with all nucleotides, high concentrations may affect cellular metabolism. Standard safety precautions for handling nucleotides should be followed, including the use of PPE and working in a fume hood.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for this compound; refer to the general safety information for similar nucleotides.
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| References | |
| Additional Infomation |
Diadenosine pentaphosphate pentaammonium is a research-grade compound used for studying purinergic signaling, cardiovascular physiology, and neurotransmission. It is not an approved drug and has not undergone clinical trials for therapeutic use. It is provided as a lyophilized powder for research use only. The compound is soluble in water (50 mg/mL) and should be stored at -20degC for long-term stability. It is classified as an endogenous metabolite and is often used as a reference standard in metabolic studies. (No additional information beyond the fields above; this compound is strictly a research tool with no clinical development.)
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| Molecular Formula |
C20H44N15O22P5
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|---|---|
| Molecular Weight |
1001.52
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| Exact Mass |
425.006
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| CAS # |
102783-61-9
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| Related CAS # |
Diadenosine pentaphosphate pentasodium;4097-04-5;Diadenosine pentaphosphate pentalithium;94108-02-8
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| PubChem CID |
177671702
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
1394.9ºC at 760 mmHg
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| Flash Point |
797.4ºC
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| Vapour Pressure |
0mmHg at 25°C
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| LogP |
1.484
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| Hydrogen Bond Donor Count |
16
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
62
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| Complexity |
1580
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C1=NC(=C2C(=N1)N(C=N2)[C@H]3[C@H](C([C@H](O3)COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@@H]4[C@@H](C([C@@H](O4)N5C=NC6=C(N=CN=C65)N)O)O)O)O)N.N.N.N.N.N
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| InChi Key |
XCOZIAOMHASKGR-ISJSRZQYSA-N
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| InChi Code |
InChI=1S/C20H29N10O22P5.5H3N/c21-15-9-17(25-3-23-15)29(5-27-9)19-13(33)11(31)7(47-19)1-45-53(35,36)49-55(39,40)51-57(43,44)52-56(41,42)50-54(37,38)46-2-8-12(32)14(34)20(48-8)30-6-28-10-16(22)24-4-26-18(10)30;;;;;/h3-8,11-14,19-20,31-34H,1-2H2,(H,35,36)(H,37,38)(H,39,40)(H,41,42)(H,43,44)(H2,21,23,25)(H2,22,24,26);5*1H3/t7-,8-,11+,12?,13?,14+,19-,20-;;;;;/m1...../s1
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| Chemical Name |
[[(2R,3R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[[(2R,4S,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate;azane
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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) |
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 | 0.9985 mL | 4.9924 mL | 9.9848 mL | |
| 5 mM | 0.1997 mL | 0.9985 mL | 1.9970 mL | |
| 10 mM | 0.0998 mL | 0.4992 mL | 0.9985 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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