| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Target: A1 adenosine receptor[1]
Tecadenoson targets the adenosine A1 receptor, where it acts as a potent and selective agonist. It has a Ki of 6.5 nM for the adenosine A1 receptor and is selective for A1 over A2 receptors (Ki = 2,315 nM). By activating A1 receptors in the heart, tecadenoson slows atrioventricular conduction and reduces heart rate, making it useful for the treatment of supraventricular tachyarrhythmias. |
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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].
In vitro, tecadenoson is a potent adenosine A1 receptor agonist with a Ki of 6.5 nM. It is selective for adenosine A1 over A2 receptors (Ki = 2,315 nM). The compound prolongs stimulus-His bundle potential (SH) intervals in isolated perfused guinea pig hearts with an EC50 of 40.6 nM, confirming its functional activity at cardiac A1 receptors. |
| 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].
In vivo, tecadenoson induces PR interval prolongation in anesthetized guinea pigs with an ED50 of 0.9 μg/kg. It reduces heart rate in anesthetized rats in a dose-dependent manner without affecting blood pressure. These in vivo effects are consistent with its mechanism as an adenosine A1 receptor agonist, slowing atrioventricular conduction and reducing heart rate while maintaining hemodynamic stability. |
| Enzyme Assay |
In vitro receptor binding assays for tecadenoson measure its affinity for adenosine A1 and A2 receptors using radioligand displacement techniques. Membranes prepared from cells expressing the receptors are incubated with a radiolabeled adenosine receptor ligand and varying concentrations of the compound. The binding affinity (Ki = 6.5 nM for A1; Ki = 2,315 nM for A2) is calculated from competitive binding curves. Functional assays measure receptor activation via cAMP accumulation or other downstream readouts.
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| Cell Assay |
In vitro cell-based assays for tecadenoson use cells expressing adenosine A1 or A2 receptors. Cells are treated with serial dilutions of the compound, and receptor activation is measured by assessing changes in cAMP levels or other signaling readouts. The EC50 for receptor activation is calculated from dose-response curves. The compound's selectivity for A1 over A2 receptors is confirmed by comparing EC50 values in cells expressing each receptor subtype.
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| Animal Protocol |
Rat: The effects of Tecadenoson on heart rate and to reduce serum NEFA concentration are determined in separate groups of rats to avoid the effects of animal handling and blood sampling on heart rate. Three days before an experiment, a catheter (0.025-mm outer diameter) is implanted in the left common carotid artery of each rat using aseptic conditions and sterile technique. The catheter is tunneled subcutaneously to the dorsal surface. After recovery from anesthesia, rats are placed in metabolic cages to facilitate handling and blood sampling. Blood samples (0.2 mL) are drawn before and at various time points after i.p. injection of either Tecadenoson or vehicle (DMSO in saline). A 0.4-mL volume of 1% sodium citrate in saline is administered after withdrawal of each blood sample to replace blood volume and prevent clotting in the carotid artery catheter. Serum is collected from each sample after centrifugation of the clotted blood. Serum samples are stored at 80°C until analysis. Serum NEFA concentration is determined using an enzymatic colorimetric assay kit[2]. |
| ADME/Pharmacokinetics |
Tecadenoson has a molecular formula of C14H19N5O5 and a molecular weight of 337.33. The compound is soluble in DMF at 30 mg/mL, in DMSO at 30 mg/mL, and partially soluble in ethanol. It is stored at -20°C and shipped at room temperature. The compound is administered intravenously in preclinical and clinical studies. Pharmacokinetic parameters including half-life and clearance are documented in research publications.
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| Toxicity/Toxicokinetics |
The toxicity profile of tecadenoson has been characterized in preclinical safety studies. As an adenosine A1 receptor agonist, the compound may cause bradycardia and AV block at high doses. The compound is for research use only and is not for human or veterinary use. Appropriate safety precautions should be taken during handling. The safety margin and no-observed-adverse-effect level (NOAEL) are determined from toxicology studies.
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| References |
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| Additional Infomation |
Tecadenoson is a novel selective A1 adenosine receptor agonist currently being evaluated for its efficacy in converting paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm. It was developed by CV Therapeutics, Inc. Drug Indications It is being investigated for the treatment of arrhythmias and atrial fibrillation. Mechanism of Action Tecadenoson selectively stimulates A1 adenosine receptors. Stimulation of A1 adenosine receptors slows electrical impulse conduction in the atrioventricular node (the region that controls the conduction of electrical impulses from the atria to the ventricles). Pharmacodynamics Tecadenoson is a novel A1 adenosine receptor agonist. Adenosine is a natural compound that stimulates all adenosine receptor subtypes in the body, including the A2 adenosine receptor, which can lower blood pressure. In non-clinical trials, ticanosone selectively stimulates A1 adenosine receptors in the atrioventricular node, slowing the electrical conduction velocity of the atrioventricular node, reducing the number of electrical impulses reaching the ventricles, without affecting blood pressure. Clinical studies of intravenously administered ticanosone to date suggest that it may slow atrioventricular node conduction velocity by selectively stimulating A1 adenosine receptors and avoid lowering blood pressure by not stimulating A2 adenosine receptors. Therefore, intravenous ticanosone may be used to convert patients with paroxysmal supraventricular tachycardia (PSVT) to a normal sinus rhythm without lowering blood pressure or causing adverse reactions related to vasodilation, such as flushing, palpitations, or headache.
Tecadenoson is also known by the synonym CVT-510. It was developed by CV Therapeutics for the treatment of paroxysmal supraventricular tachycardia and for rate control in atrial fibrillation and atrial flutter. The compound is a selective adenosine A1 receptor agonist with a Ki of 6.5 nM. It is used primarily for research purposes and is not approved for clinical use. |
| 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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