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PRODUCT INFORMATION Proxyphylline Item No. 20937

CAS Registry No.: 603-00-9 Formal Name: 3,7-dihydro-7-(2-hydroxypropyl)-1,3- N dimethyl-1H-purine-2,6-dione O N Synonym: NSC 163343 C H N O MF: 10 14 4 3 N FW: 238.2 N

Purity: ≥98% O UV/Vis.: λmax: 273, 324 nm Supplied as: A crystalline solid OH Storage: -20°C Stability: As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly

Laboratory Procedures

Proxyphylline is supplied as a crystalline solid. A stock solution may be made by dissolving the proxyphylline in the solvent of choice. Proxyphylline is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of proxyphylline in ethanol is approximately 1 mg/ml and approximately 10 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of proxyphylline can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of proxyphylline in PBS, pH 7.2, is approximately 1 mg/ml. We do not recommend storing the aqueous solution for more than one day.

Description

Proxyphylline is a methylxanthine derivative that has bronchodilatory actions.1 It has also been reported 2 to have vasodilatory and cardiac stimulatory effects. Proxyphylline selectively antagonizes A1 adenosine 3 receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets). Proxyphylline has been mixed with Melilotus extract to generate a theo-esberiven product, which can have cardiovascular and anti-allodynia effects in mammals.2,4

References

1. Rasmussen, F.V., Waldorff, S., and Madsen, L. Pharmacokinetics and bronchodilatory effect of proxyphylline and theophylline. Eur. J. Respir. Dis. 65(1), 20-27 (1984). 2. Takeda, K., Katano, Y., Nakagawa, Y., et al. Effects of aminophylline, proxyphylline and a proxyphylline-Melilotus extract-rutin mixture (theoesberiven) on the heart and the coronary circulation. Jpn. J. Pharmacol. 27(5), 709-720 (1977). 3. Schwabe, U., Ukena, D., and Lohse, M.J. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn-Schmiedeberg’s Arch. Pharmacol. 330, 212-221 (1985). 4. Bang, S., Kim, Y.S., and Jeong, S.R. Anti-allodynic effect of theoesberiven F in a vincristine-induced neuropathy model. Exp. Ther. Med. 12(2), 799-803 (2016).

WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897

WARRANTY AND LIMITATION OF REMEDY [734] 971-3335 Buyer agrees to purchase the material subject to Cayman’s Terms and Conditions. Complete Terms and Conditions including Warranty and Limitation of Liability information can be found on our website. FAX: [734] 971-3640 [email protected] Copyright Cayman Chemical Company, 12/22/2016 WWW.CAYMANCHEM.COM