WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 328401
CAS#: 603-00-9
Description: Proxyphylline is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.
MedKoo Cat#: 328401
Name: Proxyphylline
CAS#: 603-00-9
Chemical Formula: C10H14N4O3
Exact Mass: 238.1066
Molecular Weight: 238.247
Elemental Analysis: C, 50.41; H, 5.92; N, 23.52; O, 20.15
Synonym: Proxyphylline; NSC 163343; NSC163343; NSC-163343;
IUPAC/Chemical Name: 7-(2-hydroxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
InChi Key: KYHQZNGJUGFTGR-UHFFFAOYSA-N
InChi Code: InChI=1S/C10H14N4O3/c1-6(15)4-14-5-11-8-7(14)9(16)13(3)10(17)12(8)2/h5-6,15H,4H2,1-3H3
SMILES Code: O=C(N1C)N(C)C2=C(N(CC(O)C)C=N2)C1=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 238.247 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Borowiecki P, Paprocki D, Dudzik A, Plenkiewicz J. Chemoenzymatic Synthesis of Proxyphylline Enantiomers. J Org Chem. 2016 Jan 15;81(2):380-95. doi: 10.1021/acs.joc.5b01840. Epub 2016 Jan 6. PubMed PMID: 26517306.
2: Soulas DN, Sanopoulou M, Papadokostaki KG. Proxyphylline release kinetics from symmetrical three-layer silicone rubber matrices: effect of different excipients in the outer rate-controlling layers. Int J Pharm. 2012 May 10;427(2):192-200. doi: 10.1016/j.ijpharm.2012.01.056. Epub 2012 Feb 6. PubMed PMID: 22330934.
3: Ruud-Christensen M, Aasen AJ, Rasmussen KE, Salvesen B. High-performance liquid chromatographic determination of (R)-and (S)-proxyphylline in human plasma. J Chromatogr. 1989 Jul 21;491(2):355-66. PubMed PMID: 2808621.
4: Kukovetz WR, Pöch G, Holzmann S. Overadditive synergism between theophylline, diprophylline and proxyphylline in tracheal smooth muscle relaxation. Arzneimittelforschung. 1983;33(10):1450-4. PubMed PMID: 6316994.
5: Kanto J, Allonen H, Kulmala T, Mäntylä R, Tala E. Interaction between proxyphylline and salbutamol. Int J Clin Pharmacol Ther Toxicol. 1981 Aug;19(8):346-9. PubMed PMID: 7030976.
6: Rasmussen FV, Waldorff S, Madsen L. Pharmacokinetics and bronchodilatory effect of proxyphylline and theophylline. Eur J Respir Dis. 1984 Jan;65(1):20-7. PubMed PMID: 6705854.
7: Selvig K, Bjerve KS. Inhibition of human lung cyclic nucleotide phosphodiesterases by proxyphylline, theophylline and their metabolites. Acta Pharmacol Toxicol (Copenh). 1982 Sep;51(3):250-2. PubMed PMID: 6291318.
8: Tarrus E, Garcia I, Segura J. Human metabolism of 7-substituted theophyllines: N3-demethylation and lack of oxidation of proxyphylline. J Pharm Sci. 1981 May;70(5):542-5. PubMed PMID: 6894619.
9: Selvig K, Bjerve KS. Metabolism of proxyphylline in man. Isolation and identification of metabolites in urine. Drug Metab Dispos. 1980 Nov-Dec;8(6):456-62. PubMed PMID: 6109616.
10: Agbaba D, Zivanov-Stakić D, Vukićević N. Dissolution assay of theophylline, diprophylline and proxyphylline from a sustained release dosage form by high performance thin layer chromatography. Biomed Chromatogr. 1992 May-Jun;6(3):141-2. PubMed PMID: 1525489.
