| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
APNEA targets adenosine receptors, specifically A1 and A3 subtypes. By activating A1 receptors, it inhibits adenylate cyclase activity. As an A3 receptor agonist, it modulates various signaling pathways. It is a non-selective agonist, meaning it activates multiple adenosine receptor subtypes.
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| ln Vitro |
APNEA (N6-[2-(4-aminophenyl)ethyl]adenosine) is a non-selective agonist of adenosine A3 receptors that greatly increases phenidate at a subprotective dose of 1 mg/kg. Bital, diphenylhydantoin, and valproic acid can withstand maximal shock but are ineffective at lesser levels. APNEA (0.0039-1 mg/kg) similarly increases carbamazepine's protective effect. Low dosages of APNEA are anticipated to increase the protective action of carbamazepine via subtype A adenosine receptors. At higher doses, APNEA appears to enhance the anticonvulsant activity of other antiepileptic medicines via the adenosine A1 receptor [1].
In vitro, APNEA is characterized by its potent agonist activity at adenosine receptors. It has a high affinity for A1 and A3 receptors. Its activity is confirmed in functional assays where it inhibits adenylate cyclase or modulates other downstream signaling pathways. It is used to study the role of adenosine receptors in various cellular processes. |
| ln Vivo |
In amygdala-ignited rats, APNEA (N6-[2-(4-aminophenyl)ethyl]adenosine; 2-4 mg/kg) exhibited no discernible influence on seizure parameters (seizure intensity, seizure duration, and post-discharge). Anti-epileptic medications were combined with N6-[2-(4-Aminophenyl)ethyl]adenosine at levels that did not work in animals that had fully developed epilepsy [1].
In vivo, APNEA has been shown to have anticonvulsant effects. At a subprotective dose of 1 mg/kg, it significantly potentiates the anticonvulsive action of phenobarbital, diphenylhydantoin, and valproate against maximal electroshock. It also enhances the protective activity of carbamazepine. It is used in research related to ischemia, pain modulation, and central nervous system disorders. |
| Enzyme Assay |
The in vitro receptor binding assay for APNEA involves competitive binding studies using membranes from cells expressing adenosine A1 or A3 receptors. The compound is incubated with a radiolabeled ligand, such as [3H]-DPCPX or [3H]-MRS1220. The amount of radioligand displaced is measured to determine the binding affinity (Ki).
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| Cell Assay |
In vitro cell-based functional assays for APNEA utilize cells expressing adenosine receptors, such as CHO cells transfected with A1 or A3 receptors. Cells are treated with the compound, and the inhibition of adenylate cyclase activity (for A1) or the modulation of calcium mobilization (for A3) is measured. The EC50 is calculated from the concentration-response curve.
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| Animal Protocol |
In vivo animal experiments for APNEA have been performed in models of epilepsy. In these studies, the compound is administered, and its anticonvulsant effect is assessed by measuring the threshold for maximal electroshock or the severity of seizures. Its effects on pain are studied in models of nociception.
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| ADME/Pharmacokinetics |
APNEA has a molecular formula of C18H22N6O4 and a molecular weight of 386.41 g/mol. It is a solid compound that is soluble in DMSO (150 mg/mL). It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. It is a cell-permeable compound.
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| Toxicity/Toxicokinetics |
Toxicological data for APNEA are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its potent adenosine receptor agonism suggests it could have significant cardiovascular and neurological effects.
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| References |
[1]. Borowicz KK, et al. N6-2-(4-aminophenyl)ethyl-adenosine enhances the anticonvulsive activity of antiepileptic drugs. Eur J Pharmacol. 1997 May 30;327(2-3):125-133.
[2]. Borowicz KK, et al. N(6)-2-(4-aminophenyl)ethyl-adenosine enhances the anticonvulsive action of conventional antiepileptic drugs in the kindling model of epilepsy in rats. Eur Neuropsychopharmacol. 2000 Jul;10(4):237-243. |
| Additional Infomation |
APNEA is a research compound with no clinical approval. It is a valuable tool for studying adenosine receptor biology and the role of adenosine in various physiological and pathological processes. It is used in drug discovery programs to explore the therapeutic potential of adenosine receptor modulators for the treatment of epilepsy, pain, ischemia, and other neurological and cardiovascular disorders.
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| Molecular Formula |
C18H22N6O4
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|---|---|
| Molecular Weight |
386.40508
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| Exact Mass |
386.17
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| CAS # |
89705-21-5
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| PubChem CID |
9952135
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.65g/cm3
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| Boiling Point |
781.8ºC at 760 mmHg
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| Flash Point |
426.6ºC
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| Index of Refraction |
1.775
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| LogP |
0.328
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
509
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| Defined Atom Stereocenter Count |
4
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| SMILES |
N(C1=NC=NC2N([C@H]3[C@H](O)[C@H](O)[C@@H](CO)O3)C=NC1=2)CCC1C=CC(N)=CC=1
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| InChi Key |
XTPOZVLRZZIEBW-SCFUHWHPSA-N
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| InChi Code |
InChI=1S/C18H22N6O4/c19-11-3-1-10(2-4-11)5-6-20-16-13-17(22-8-21-16)24(9-23-13)18-15(27)14(26)12(7-25)28-18/h1-4,8-9,12,14-15,18,25-27H,5-7,19H2,(H,20,21,22)/t12-,14-,15-,18-/m1/s1
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| Chemical Name |
(2R,3R,4S,5R)-2-[6-[2-(4-aminophenyl)ethylamino]purin-9-yl]-5-(hydroxymethyl)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 : ~250 mg/mL (~646.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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 25.0 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.38 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.38 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 | 2.5879 mL | 12.9396 mL | 25.8792 mL | |
| 5 mM | 0.5176 mL | 2.5879 mL | 5.1758 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5879 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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