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Tecadenoson (CVT-510) is a novel and potent adenosine A1 receptor agonist (ADORA1) with the potential to be used for the treatment of paroxysmal supraventricular tachycardia. Tecadenoson appears to be an effective agent for producing rapid and sustained conversion of PSVT to sinus rhythm.
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| ln Vitro |
Tecadenoson is almost five times more effective in the atrial-paced isolated heart to extend the stimulus-to-His bundle (SH interval)—a measure of delaying AV nodal conduction—than it is to increase coronary conductance (EC50= 200 nM). Tecadenoson (40 nM) and diltiazem (1 μM) at dosages that result in an equivalent extension of the SH interval (about 10 ms) elicit a notable increase in coronary conductance and a significant decrease in left ventricular developed pressure (LVP), but Tecadenoson does not. Tecadenoson reduces ventricular monophasic action potentials (MAP) but not atrial (EC50=73 nM)[1].
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| ln Vivo |
Intravenous infusions of Tecadenoson and diltiazem extend the PR interval in atrial-paced anesthetized guinea pigs almost equally[1]. At levels that do not induce bradycardia, tecenoson (2, 5, 20 μg/kg ip) rapidly and persistently reduces NEFA. When administered at 50 μg/kg, tecanoson significantly reduces heart rate by 50% within 25 minutes, resulting in bradycardia[2].
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| Additional Infomation |
Tecadenoson is a novel selective A1 adenosine receptor agonist that is currently being evaluated for the conversion of paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm. It is being developed by CV Therapeutics, Inc.
Drug Indication Investigated for use/treatment in arrhythmia and atrial fibrillation. Mechanism of Action Tecadenoson selectively stimulates the A1 adenosine receptor. Stimulation of the A1 adenosine receptor slows the conduction of electrical impulses in the AV node of the heart, a region that controls the transmission of electrical impulses from the atria to the ventricles. Pharmacodynamics Tecadenoson is a novel A1 adenosine receptor stimulator. Adenosine is a naturally occurring compound that stimulates all adenosine receptor subtypes in the body, including the A2 adenosine receptor which lowers blood pressure. In non-clinical trials, tecadenoson selectively stimulated the A1 adenosine receptor in the AV node and slowed the speed of electrical conduction across the AV node, reducing the number of electrical impulses that reached the ventricle, without affecting blood pressure. Clinical studies to date with intravenous tecadenoson suggest that it may slow the speed of AV nodal conduction by selectively stimulating the A1 adenosine receptor, and may avoid blood pressure lowering by not stimulating the A2 adenosine receptor. Thus, it may be possible to use intravenous tecadenoson to convert patients from PSVT to normal sinus rhythm without lowering blood pressure or causing adverse events related to vasodilitation such as flushing, palpitations or headache. |
| Molecular Formula |
C14H19N5O5
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|---|---|
| Molecular Weight |
337.336
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| Exact Mass |
337.139
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| CAS # |
204512-90-3
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| PubChem CID |
158795
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| Appearance |
White to off-white solid powder
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| Density |
1.89g/cm3
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| Boiling Point |
704.9ºC at 760 mmHg
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| Flash Point |
380.1ºC
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| Vapour Pressure |
7.4E-21mmHg at 25°C
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| Index of Refraction |
1.83
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| LogP |
-0.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
446
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1COC[C@@H]1NC2=C3C(=NC=N2)N(C=N3)[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O
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| InChi Key |
OESBDSFYJMDRJY-BAYCTPFLSA-N
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| InChi Code |
InChI=1S/C14H19N5O5/c20-3-8-10(21)11(22)14(24-8)19-6-17-9-12(15-5-16-13(9)19)18-7-1-2-23-4-7/h5-8,10-11,14,20-22H,1-4H2,(H,15,16,18)/t7-,8-,10-,11-,14-/m1/s1
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| Chemical Name |
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-[[(3R)-oxolan-3-yl]amino]purin-9-yl]oxolane-3,4-diol
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| Synonyms |
CVT 510 CVT-510 Tecadenoson
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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 : ~200 mg/mL (~592.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.82 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 50.0 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: ≥ 5 mg/mL (14.82 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 50.0 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (14.82 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 | 2.9644 mL | 14.8218 mL | 29.6437 mL | |
| 5 mM | 0.5929 mL | 2.9644 mL | 5.9287 mL | |
| 10 mM | 0.2964 mL | 1.4822 mL | 2.9644 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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