While most drug metabolism is shown to happen in the liver, other organs contain drug-metabolizing enzymes and extrahepatic metabolism can play an important part in the ADME (Absorption, Distribution, Metabolism, and Excretion) profile of a drug candidate.
Human Extrahepatic Subcellular Fractions
Pooled human lung cell fractions are available, including matching (from the same donor pool) microsomes, S9, and cytosol. Some studies can yield different results between assays using smoking and non-smoking donors due to differences in enzymatic activity, so we offer subcellular fraction options from both smoking and non-smoking donors.
We offer pooled human kidney cell fractions expressing relatively high levels of CYP4A and CYP4B enzymes, efflux transporter P-glycoprotein (MDR1), and phase II drug-metabolizing enzymes including UGT1A6, UGT2B7, SULT1C2, and DT-diaphorase (NQO1). We offer microsomal, S9, and cytosolic subcellular fractions of the highest quality, specially prepared to maintain high levels of enzymatic activity.
Subcellular Fractions in Preclinical Drug Development
Our subcellular offerings are prepared using methods to ensure the highest quality with regards to function and enzymatic activity. Fractions can be used in metabolism studies to study how a drug’s disposition is affected by interaction with enzymes outside of the liver. For example, esterase is a drug-metabolizing enzyme highly expressed in intestinal cytosol and can be investigated using enteric cytosolic fraction as a test system in a metabolism study. For therapeutics that may be administered in breathing treatments or through dermal patches, lung or skin fractions may be more appropriate to properly identify enzymes interacting with a drug before it gets absorbed into the bloodstream.
Don’t see what you need? Other preparations can be made available!
If you require subcellular fractions not listed in our standard product offerings, custom preparations can be easily ordered to meet the specific needs of any study. Our team of specialists is highly experienced with an extensive battery of characterization assays, unusual tissues and fractions, and a wide variety of animal species. See all of our Custom Products capabilities or get in touch with a specialist to find out how we can help.