| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
| ln Vivo |
Treatment with PD 117519 (2–10 mg/kg; oral; 16–24 hours) resulted in significant hemodynamic alterations in male beagle dogs at Tmax (4 hours) and 16 hours after the dose. acute damage to the coronary arteries. At the time of maximum drug exposure (4 hours postdose), treatment with 2 or 10 mg/kg of PD 117519 significantly raised mean heart rate and lowered mean indirect systolic blood pressure [3].
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|---|---|
| Animal Protocol |
Animal/Disease Models: 24 male beagle dogs (8-12 months old) [3]
Doses: 2 mg/kg or 10 mg/kg Route of Administration: Oral; 16-hour and 24-hour Experimental Results: At peak drug exposure, avg. Heart rate increases and mean indirect systolic blood pressure decreases. Induce acute coronary artery disease. Endothelial cells are also damaged. |
| References |
[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.
[2]. Tobin GA, et al. The role of eNOS phosphorylation in causing drug-induced vascular injury. Toxicol Pathol. 2014 Jun;42(4):709-24. [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. |
| Additional Infomation |
See also: N-(2,3-dihydro-1H-inden-1-yl)adenosine (annotation moved to).
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| Molecular Formula |
C19H21N5O4
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|---|---|
| Molecular Weight |
383.40114
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| Exact Mass |
383.159
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| CAS # |
96392-15-3
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| PubChem CID |
13424663
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.71g/cm3
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| Boiling Point |
723.3ºC at 760 mmHg
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| Flash Point |
391.2ºC
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| Index of Refraction |
1.821
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| LogP |
0.61
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
556
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C=NC2C(=NC=NC1=2)N[C@@H]1CCC2C=CC=CC1=2
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| InChi Key |
FSKMJUWPFLDDRS-BYMDKACISA-N
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| InChi Code |
InChI=1S/C19H21N5O4/c25-7-13-15(26)16(27)19(28-13)24-9-22-14-17(20-8-21-18(14)24)23-12-6-5-10-3-1-2-4-11(10)12/h1-4,8-9,12-13,15-16,19,25-27H,5-7H2,(H,20,21,23)/t12-,13-,15-,16-,19-/m1/s1
|
| Chemical Name |
(2R,3R,4S,5R)-2-[6-[[(1R)-2,3-dihydro-1H-inden-1-yl]amino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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| Synonyms |
PD117519; PD 117519; PD-117519; CI947; CI 947; CI-947
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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 : ≥ 100 mg/mL (~260.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 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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