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S9 Metabolic Stability Assay

Creative Animodel is a leading biotech company, specializing in offering a set of services for extensive drug metabolism and pharmacokinetic capabilities. We provide liver S9 stability study to investigate in vitro intrinsic clearance of new drug candidates. Our experienced scientists and advanced techniques enable us to deliver consistent and high-quality data with cost-efficiency.

Why Choose S9 Fraction?

The liver is regarded as the major site of drug metabolism in humans and animals, where the enzymes catalyzing drug metabolism reactions are located mainly in the microsomes and soluble fraction of the cytoplasma. Microsomes contain the cytochrome P450 isoforms (CYPs) and cytosolic portion contains major part of transferases. S9 fraction is a kind of subcellular fractions obtained from liver homogenate by centrifugation. And S9 fraction is highly enriched in both microsomal and cytosolic enzymes, providing a wide variety of both Phase I and Phase II enzymes. Presently, hepatic S9 fraction is an experimental in vitro system frequently used for understanding metabolic parameters of xenobiotics.

Applications:
• Metabolic stability evaluating
Metabolite profiling
Advantages:
• Easy to prepare, use and store
• Containing both Phase I and II enzymes
• Capable of investigating Phase II metabolic pathways (supplemented with
   cofactors such as UDPGA and PAPS)
• Cost-efficient over whole cell models.

How Is S9 Metabolic Stability Assay performed?

Liver S9 fraction is obtained from human and various animal species including but not restricted to primate, pig, dog, rabbit, rat and mouse. Test compounds are incubated with S9 fraction at 37℃ in duplicate. We also afford Phase I or combined Phase I/Phase II assay to determine both Phase I and Phase II metabolism by utilizing cofactors NADPH and UDPGA. After incubation, the supernatant is collected by centrifugation, and the concentration of parent compound is investigated by LC-MS/MS analysis at five-time points over 60 minutes (0, 15, 30, 45 and 60 min, or customized). Data output consists of mean intrinsic clearance and half-life measurements.

Figure 2. S9 Stability data for 7-hydroxycoumarin in the presence of cofactors. Data are shown as mean ± standard deviation.

Creative Animodel provides a wide variety of in vitro metabolic stability studies for metabolic investigation of novel drugs in a fast and cost-efficient manner. By understanding the metabolic profiles, we offer our clients the information necessary to make chemical and structural optimization for increasing drug efficacy and decreasing toxicities. If you have any questions or specific requirements, please do not hesitate to contact us.

References:
1. Jia L, Liu X. The Conduct of Drug Metabolism Studies Considered Good Practice (II): In Vitro Experiments. Curr Drug Metab. 2007 Dec; 8(8): 822–829.
2. Samantha J. Richardson, et al. Efficiency in Drug Discovery: Liver S9 Fraction Assay As a Screen for Metabolic Stability. Drug Metab Lett. 2016 May; 10(2): 83–90.

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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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