PD 117519
Based on 1 Customer Validation
PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
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- Reinheit: 99.94%
- CAS. Nr.: 96392-15-3
- Formel: C19H21N5O4
- Molecular Weight:383.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
A2A adenosine[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:24 male beagle dogs (8-12 months old)[3]
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Dosage:2 mg/kg or 10 mg/kg
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Administration:Oral administration; 16 hours and 24 hours
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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.
Chemical Information
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CAS. Nr. 96392-15-3
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Appearance Solid
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Molecular Weight 383.40
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Formel C19H21N5O4
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Color White to off-white
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SMILES
OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@@H]1N2C=NC3=C2N=CN=C3NC4CC(C=CC=C5)=C5C4
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Synonyms
CI947
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Reynolds DL, et al. Liquid chromatographic analysis of the adenosine agonist PD 117519 in dog plasma. J Pharm Biomed Anal. 1991;9(4):345-9. [Content Brief]
[2]. Tobin GA, et al. The role of eNOS phosphorylation in causing drug-induced vascular injury. Toxicol Pathol. 2014 Jun;42(4):709-24. [Content Brief]
[3]. Enerson BE, et al. Acute drug-induced vascular injury in beagle dogs: pathology and correlating genomic expression. Toxicol Pathol. 2006;34(1):27-32. [Content Brief]
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 |