2. GPCR/G Protein
  3. Adenosine Receptor
  4. Tecadenoson

Tecadenoson  (Synonyms: CVT-510)

Cat. No.: HY-19661 Purity: 99.76%
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Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.

For research use only. We do not sell to patients.

Tecadenoson Chemical Structure

Tecadenoson Chemical Structure

CAS No. : 204512-90-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Tecadenoson Related Antibodies

Top Publications Citing Use of Products

View All Adenosine Receptor Isoform Specific Products:

View All Isoforms
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.

IC50 & Target

Target: A1 adenosine receptor[1]
In Vitro

In the atrial-paced isolated heart, Tecadenoson is approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50=41 nM) than to increase coronary conductance (EC50=200 nM). At concentrations of Tecadenoson (40 nM) and diltiazem (1 μM) that causes equal prolongation of S-H interval (∼10 ms), diltiazem, but not Tecadenoson, significantly reduces left ventricular developed pressure (LVP) and markedly increases coronary conductance. Tecadenoson shortens atrial (EC50=73 nM) but not the ventricular monophasic action potentials (MAP)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tecadenoson Related Antibodies
In Vivo

In atrial-paced anaesthetized guinea-pigs, intravenous infusions of Tecadenoson and diltiazem causes nearly equal prolongations of P-R interval[1]. Tecadenoson (2, 5, 20 μg/kg i.p.) causes a rapid and sustained dose-dependent decrease in NEFA at doses that do not cause bradycardia. Tecadenoson given at 50 μg/kg causes a significant bradycardia (50% decrease in heart rate at 25 min[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

337.33

Formula

C14H19N5O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2N=CN=C3N[C@H]4COCC4)O1)O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (592.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9645 mL 14.8223 mL 29.6446 mL
5 mM 0.5929 mL 2.9645 mL 5.9289 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

The effect of Tecadenoson on binding to A1 and A2A-adenosine receptors of porcine forebrain and striatum membranes, respectively, are determined. Assays for A1 and A2A receptors are carried out by using the A1 receptor antagonist [3H]CPX and the A2A receptor agonist [3H]CGS 21680. Membranes are treated with adenosine deaminase (2 U/mL) for 20 min at room temperature prior to and during radioligand binding assays. Membranes (0.2-0.7 mg), adenosine deaminase, and the indicated radioligand are incubated for 3 h in a 300 μL volume of Tris-HCl buffer (50 mM) (pH 7.4). Assays are carried out in triplicate at room temperature. After the incubation period, bound and free radioligand are diluted by the addition of ice-cold Tris-HCl buffer (5 mL), and immediately separated by vacuum filtration of assay contents onto Whatman GF/C filters and ishing of trapped membranes with Tris-HCl buffer (20 mL). Filter disks containing membrane-bound radioactivity are placed in 4 mL Scintiverse, and the radioactivity is quantified by a liquid scintillation counter. Specific binding of [3H]CPX and [3H]CGS 21680 is defined as membrane binding displaced in the presence of CPT (10 μM) and R-PIA (10 μM), respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9645 mL 14.8223 mL 29.6446 mL 74.1114 mL
5 mM 0.5929 mL 2.9645 mL 5.9289 mL 14.8223 mL
10 mM 0.2964 mL 1.4822 mL 2.9645 mL 7.4111 mL
15 mM 0.1976 mL 0.9882 mL 1.9763 mL 4.9408 mL
20 mM 0.1482 mL 0.7411 mL 1.4822 mL 3.7056 mL
25 mM 0.1186 mL 0.5929 mL 1.1858 mL 2.9645 mL
30 mM 0.0988 mL 0.4941 mL 0.9882 mL 2.4704 mL
40 mM 0.0741 mL 0.3706 mL 0.7411 mL 1.8528 mL
50 mM 0.0593 mL 0.2964 mL 0.5929 mL 1.4822 mL
60 mM 0.0494 mL 0.2470 mL 0.4941 mL 1.2352 mL
80 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9264 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7411 mL
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Tecadenoson Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tecadenoson204512-90-3CVT-510CVT510CVT 510Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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