2. GPCR/G Protein
  3. Adenosine Receptor
  4. PD 117519

PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.

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PD 117519 Chemical Structure

PD 117519 Chemical Structure

CAS No. : 96392-15-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

PD 117519 Related Antibodies

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View All Adenosine Receptor Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models[1][2].

IC50 & Target

A2A adenosine[1]
In Vivo

PD 117519 (2-10 mg/kg; oral administration; 16-24 hours; male beagle dogs) treatment produces significant hemodynamic changes at Tmax (4 hours) follows by acute coronary vascular injury that is evident at 16 hours postdosing.Treatment with 2 or 10 mg/kg of PD 117519 produces significant increases in mean heart rate and decreases in mean indirectsystolic blood pressure at time of highest drug exposure, 4 hours postdosing[3].

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

Animal Model: 24 male beagle dogs (8-12 months old)[3]
Dosage: 2 mg/kg or 10 mg/kg
Administration: Oral administration; 16 hours and 24 hours
Result: Increased in mean heart rate and decreased in mean indirectsystolic blood pressure at time of highest drug exposure. Induced acute coronary arteriopathy. The endothelium also appears injured.
Molecular Weight

383.40

Formula

C19H21N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@@H]1N2C=NC3=C2N=CN=C3NC4CC(C=CC=C5)=C5C4
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 : ≥ 100 mg/mL (260.82 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 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.52 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: 99.97%

COA (253 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
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 2.6082 mL 13.0412 mL 26.0824 mL 65.2061 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL 13.0412 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL 6.5206 mL
15 mM 0.1739 mL 0.8694 mL 1.7388 mL 4.3471 mL
20 mM 0.1304 mL 0.6521 mL 1.3041 mL 3.2603 mL
25 mM 0.1043 mL 0.5216 mL 1.0433 mL 2.6082 mL
30 mM 0.0869 mL 0.4347 mL 0.8694 mL 2.1735 mL
40 mM 0.0652 mL 0.3260 mL 0.6521 mL 1.6302 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3041 mL
60 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8151 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6521 mL
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PD 117519 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:

PD 11751996392-15-3CI947PD117519PD-117519CI 947CI-947Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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