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| QA- GSH- Novel Agent for Reactive Metabolite Detection |
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Bioactivation of drug candidates resulting in chemically reactive, electrophilic metabolites have always presented a major challenge to pharmaceutical companies. Not only this, but the measurement of these metabolites has been hampered by the lack of an effective quantitative method. AnaSpec is pleased to introduce QA-GSH, a valuable new tool for the detection of reactive metabolites.
QA-GSH is a novel quaternary ammonium glutathione analogue conjugating agent described by Soglia, et al.1 Developed by Pfizer, this compound can provide semiquantitative assessment of the bioactivation potential in vitro. for semiquantitative LC-MS/MS detection of reactive metabolite. The methodology is well suited for use in early drug discovery high throughput screening paradigms.
N-(1-Pyrenyl)maleimide-QA-GSH ("Conjugate 6" in the paper) is also available. Contact AnaSpec (service@anaspec.com) regarding information about Tetramethylrhodamine-5-maleimido-QA-GSH ("Conjugate 7").
To request AnaSpec’s Forthcoming Combinatorial Chemistry catalog, click here.
Reference:
1. Soglia, J.R.; G. Contillo, L.G.; Kalgutkar, A.S.; Zhao, S.; Hop, C.E.C.A.; Boyd, J.G.; Cole, M.J. A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues, Chem. Res. Toxicol. 2006, 19, 480-490]
(Note: this article was one of the Chemical Research in Toxicology's top 15 most accessed articles in 2006)
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