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| ln Vitro |
In human whole blood, binodenson (MRE-0470) (30-300 nM) operates in concert with Rolipram to decrease the oxidative activity of FMLP-stimulated polymorphonuclear leukocytes caused by tumor necrosis factor-alpha [1].
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| ln Vivo |
Binodenson (infusion 0-0.9 μg/kg/h; adult Wistar rats; rat bacterial meningitis model), with or without rolipram (0-0.01 μg/kg/h), suppresses pleocytosis and lowers lipopolysaccharide-induced enhanced blood-brain barrier permeability (BBBP), indicating less neutrophil-induced damage [1].
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| Animal Protocol |
Rat Bacterial Meningitis Model:** Adult Wistar rats were anesthetized with ketamine and xylazine. Meningitis was induced via intracisternal inoculation of LPS (200 ng) from *E. coli*. Test compounds (WRC-0470 and/or rolipram) were infused intravenously over the duration of the experiment using a Harvard pump. At 4 hours post-inoculation, cerebrospinal fluid (CSF) and blood were sampled. CSF white blood cell (WBC) counts were determined by hemocytometer. For assessment of blood-brain barrier permeability (BBBP), rats received an intravenous injection of ¹²⁵I-labeled BSA at the time of intracisternal inoculation. The percentage of BBBP was calculated as (cpm in CSF / cpm in blood) × 100 [1].
* **Determination of WRC-0470 Plasma Concentrations:** A sensitive radioreceptor assay was developed using the high-affinity binding of WRC-0470 to recombinant A₂A receptors. Plasma samples were first purified on C18 Sepaks to remove interfering compounds. The eluted samples were then tested in the radioligand binding assay, and drug concentrations were derived from a standard curve [1]. |
| ADME/Pharmacokinetics |
Biological Half-Life
10 ± 4 minutes |
| References |
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| Additional Infomation |
Binodenoson is a pharmacological stress test agent that specifically targets the A2A receptor, the only adenosine receptor essential for increasing blood flow to the heart. This specificity allows Binodenoson to deliver a more effective dose of the drug with fewer side effects in a single injection compared to existing therapies, which typically require 15-20 minutes of infusion. Drug Indications For use in cardiac pharmacological stress SPECT imaging, used to diagnose coronary artery disease. Mechanism of Action Binodenoson is a highly selective adenosine A2A receptor agonist. The adenosine A2A receptor is essential for increasing blood flow to the heart, and Binodenoson's specificity to this particular receptor allows it to deliver a more effective dose of the drug with fewer side effects in a single injection compared to existing therapies, which typically require 15-20 minutes of infusion. Cardiac stress testing allows physicians to determine the presence of cardiovascular disease by examining blood flow to the heart.
Pharmacodynamics Binodenoson is a novel diagnostic agent for cardiovascular disease. It is an adenosine A2A receptor agonist and is currently being developed for cardiac pharmacological stress SPECT imaging, which is used to diagnose coronary artery disease. |
| Molecular Formula |
C17H25N7O4
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|---|---|
| Molecular Weight |
391.432
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| Exact Mass |
391.197
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| CAS # |
144348-08-3
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| PubChem CID |
9576912
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| Appearance |
White to off-white solid powder
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| Density |
1.76g/cm3
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| Boiling Point |
765.6ºC at 760mmHg
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| Flash Point |
416.8ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.812
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| LogP |
0.652
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
550
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1(/C=N/NC2=NC3=C(N=CN3C3OC(CO)C(O)C3O)C(N)=N2)CCCCC1
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| InChi Key |
XJFMHMFFBSOEPR-DNZQAUTHSA-N
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| InChi Code |
InChI=1S/C17H25N7O4/c18-14-11-15(22-17(21-14)23-20-6-9-4-2-1-3-5-9)24(8-19-11)16-13(27)12(26)10(7-25)28-16/h6,8-10,12-13,16,25-27H,1-5,7H2,(H3,18,21,22,23)/b20-6+/t10-,12-,13-,16-/m1/s1
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| Chemical Name |
(2R,3R,4S,5R)-2-[6-amino-2-[(2E)-2-(cyclohexylmethylidene)hydrazinyl]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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| Synonyms |
Binodenoson WRC-0470 WRC 0470
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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 (~319.35 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.31 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 (5.31 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 (5.31 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 | 2.5547 mL | 12.7737 mL | 25.5474 mL | |
| 5 mM | 0.5109 mL | 2.5547 mL | 5.1095 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5547 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00944970 | COMPLETED | Drug: binodenoson Drug: adenosine |
Coronary Artery Disease | Pfizer | 2005-10 | Phase 3 |
| NCT00944294 | COMPLETED | Drug: binodenoson Drug: adenosine |
Coronary Artery Disease | Pfizer | 2004-02 | Phase 3 |
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