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

Capadenoson  (Synonyms: BAY 68-4986)

Cat. No.: HY-14917 Purity: 99.62%
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Capadenoson is a selective agonist of adenosine-A1 receptor.

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

Capadenoson Chemical Structure

Capadenoson Chemical Structure

CAS No. : 544417-40-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1ML in DMSO
ready for reconstitution
 USD 85 In-stock
Solution
10 mM * 1ML in DMSO USD 85 In-stock
Solid
5 mg USD 74 In-stock
10 mg USD 110 In-stock
25 mg USD 222 In-stock
50 mg USD 333 In-stock
100 mg USD 500 In-stock
200 mg   Get quote  
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Customer Review

Based on 8 publication(s) in Google Scholar

Capadenoson 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

Capadenoson is a selective agonist of adenosine-A1 receptor.

IC50 & Target

Adenosine A1 receptor[1]
Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.1 nM
Compound: Capadenoson
Agonist activity at adenosine A1 receptor (unknown origin) expressed in CHO cells assessed as increase in intracellular cAMP level by RIA
Agonist activity at adenosine A1 receptor (unknown origin) expressed in CHO cells assessed as increase in intracellular cAMP level by RIA
[PMID: 24669958]
CHO EC50
1.1 nM
Compound: 4, page S2,26
Agonist activity at human adenosine A1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
Agonist activity at human adenosine A1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
[PMID: 26210506]
In Vitro

To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). CCPA shows a Ki value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki values in the absence and presence of GTP. Capadenson shows a Ki value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson[1].

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

Capadenoson Related Antibodies
In Vivo

In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 0.15 mg/kg for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 μg/L on day 4 and 5, respectively[1].

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

520.03

Formula

C25H18ClN5O2S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=C(C2=CC=C(OCCO)C=C2)C(C#N)=C(SCC3=CSC(C4=CC=C(Cl)C=C4)=N3)N=C1N
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 : ≥ 50 mg/mL (96.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9230 mL 9.6148 mL 19.2297 mL
5 mM 0.3846 mL 1.9230 mL 3.8459 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

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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: 2.5 mg/mL (4.81 mM); Suspended solution; Need ultrasonic and warming

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 99.62%

SDS (393 KB)

COA (246 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Membranes from the human cortex are prepared. [35S]GTPγS binding is measured. Briefly, 5 µg of membrane protein is incubated in a total volume of 160 µL for 2 hr at 25°C in a shaking water bath. [35S]GTPγS binding in control incubations and in the presence of capadenoson showed a linear time course up to this incubation time. Binding buffer contained 50 mM Tris/HCl, pH 7.4, 2 mM triethanolamine, 1 mM EDTA, 5 mM MgCl2, 10 µM GDP, 1 mM dithiothreitol, 100 mM NaCl, 0.2 units/mL adenosine deaminase, 0.2 nM [35S]GTPγS, and 0.5% bovine serum albumin. Non-specific binding is determined in the presence of 10 µM GTPγS. Incubations are terminated through filtration of the samples over multiscreen FB glass fiber filters followed by two washes with binding buffer. The filters are dried, coated with scintillator and counted for radioactivity. Binding curves of [35S]GTPγS are analyzed by nonlinear regression using GraphPad Prism[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
A total of 14 Wistar rats and 18 SHR (body weight 200-50 g, all female) underwent experiments to evaluate the exocytotic, stimulation-induced NE release during electrical field stimulation. Rats are killed by an injection of pentobarbital i.p. (0.5 mL/100 mg body weight), and hearts are rapidly excised, and placed in ice cold Krebs-Henseleit solution (KHL). They are quickly mounted on a Langendorff apparatus for retrograde perfusion with KHL. Perfusion rate is kept constant at 10 mL/min, the temperature is adjusted to 37°C, and the pH to 7.4 through bubbling with 5% CO2/95% O2. Via an inflow line desipramine at a concentration of 10−7 M is added to the perfusion buffer. After an equilibration period of 20 minutes, electrical field stimulation is commenced via two metal paddles adjacent to both sides of the beating heart for 1 minute (5V, 6 Hz). We collected the efflux in plastic tubes the minute before, during, and 3 minutes after the stimulation. These are rapidly frozen in liquid nitrogen and stored at −20°C till analysis. The NE release is calculated as the cumulative release induced by the electrical stimulation. After the first stimulation (S1), the study drug Capadenoson at concentrations of 30 µg/L (6×10−8 M) or 300 µg/L(6×10−7 M), or 2-chloro-N6-cyclopentyladenosine (CCPA, 10−6 M), respectively, are added via separate perfusion lines for 30 minutes. After this time a second stimulation (S2) is executed to determine the effect of the drugs on NE release compared to the first stimulation. The effect of each pharmacological intervention is analysed by calculating the ratio of NE release induced by the second and first stimulation (S2/S1 ratio).

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 1.9230 mL 9.6148 mL 19.2297 mL 48.0741 mL
5 mM 0.3846 mL 1.9230 mL 3.8459 mL 9.6148 mL
10 mM 0.1923 mL 0.9615 mL 1.9230 mL 4.8074 mL
15 mM 0.1282 mL 0.6410 mL 1.2820 mL 3.2049 mL
20 mM 0.0961 mL 0.4807 mL 0.9615 mL 2.4037 mL
25 mM 0.0769 mL 0.3846 mL 0.7692 mL 1.9230 mL
30 mM 0.0641 mL 0.3205 mL 0.6410 mL 1.6025 mL
40 mM 0.0481 mL 0.2404 mL 0.4807 mL 1.2019 mL
50 mM 0.0385 mL 0.1923 mL 0.3846 mL 0.9615 mL
60 mM 0.0320 mL 0.1602 mL 0.3205 mL 0.8012 mL
80 mM 0.0240 mL 0.1202 mL 0.2404 mL 0.6009 mL
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Capadenoson 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:

Capadenoson544417-40-5BAY 68-4986Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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