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DMPK

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Reactive Metabolite Analysis

Creative Animodel is a leading biotech company specializing in offering a set of services for DMPK. With years of exploration, our scientific team has gathered abundant experience and set up leading technical platforms for studying metabolite ID. Based on professional platforms and experts, our company provides the most reliable service about reactive metabolites.

What Are Reactive Metabolites?

A number of drugs were reported to undergo metabolic activation by drug-metabolizing enzymes. The bioactivation forms reactive metabolites, which readily bind to macromolecules in a covalent manner, such as proteins and DNA. Reactive metabolites can be divided into diverse groups such as epoxides, quinones, free radicals, reactive oxygen species, and unstable conjugates. Due to their high reactivity and short half-life, reactive metabolites are not directly detected by traditional analytical methods. Most reactive metabolites are electrophilic in nature and can react with nucleophiles. In in vitro microsomal incubations, small nucleophilic molecules, such as glutathione (GSH; most often used), cyanide (KCN; used for hard electrophiles) and amines (such as semicarbazide) are generally used to trap reactive metabolites. Structural elucidation of these stable adducts is conducted by liquid chromatography-tandem mass spectrometry (LC/MS).

Why Reactive Metabolite Analysis Is Important?

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Reactive metabolites are one of the main factors causing unexpected drug-induced toxicity through binding proteins or DNA. Therefore, reactive metabolites are widely regarded as playing a key role in the pathogenesis of idiosyncratic adverse drug reactions. The experiments about reactive metabolites can be conducted at any stage in the drug discovery-development continuum and are often part of the decision processing for advancing a drug candidate. Since the risk of later stage failure is the considerable financial burden of drug development, screening for reactive metabolite formation in lead optimization is emerging a common choice.

Advantages

Both hard and soft electrophiles are trapped by the use of different trapping agents. We offer a test system with different stable isotope labeled agents for trapping different types of reactive metabolites from microsomal incubations.

Superior UPLC-TOF/MS platform is provided for detection of metabolites at very low concentrations. The high mass resolution and accurate mass measurement capability of TOF/MS, with the possibility to simultaneously acquire in-source fragment ion data, enables also structural identification of the detected trapped reactive metabolites. This platform improves detection of the conjugates and allows perfect fragmentation pattern and spectrum confirmation.

Professional scientists and expert staffs analyze data to get reliable and detailed information about reactive metabolites.

Creative Animodel has been devoted to the field of reactive metabolite analysis for years. Our well-trained scientists are specialized in formulating and carrying out the most relevant plans to meet different needs. We are confident to serve customers with high-efficiency assays and high-quality data.

Our customer service representatives are available 24 hours a day, from Monday to Sunday.

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Telephone: Email: 1-631-871-5806 bd@creative-animodel.com Please fill out the form below:
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45-1 Ramsey Road, Shirley, NY 11967, USA 1-631-207-8356 1-631-871-5806 Europe 44-207-097-1828

Creative Animodel

Creative Animodel is a world's leading commercial provider of custom animal model services. We offer top-quality services at unbeatable prices. Our customer service representatives are available 24 hours a day, from Monday to Sunday.

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