Absorption Systems uses both in vitro and in vivo metabolism models to characterize the metabolic stability and metabolic fate of our customers' compounds.
We routinely run assays for our customers that determine:
| Assay | Question | Test System |
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| Metabolic stability |
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| CYP reaction phenotyping |
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| CYP induction |
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| CYP inhibition |
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| Metabolite ID |
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A description of our various metabolism related assays can be found in the Assay Data Sheets listed in the Related Literature section below. Click on the ones you want to download.
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Please contact Absorption Systems if you would like our help in determining the metabolic profile of your compounds.
This assay is used to determine the stability of test compound in blood plasma for various species, including humans.
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This assay is used to determine the stability of a test compound in whole blood or plasma from mouse, rat, rabbit, dog, monkey, or human.
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This assay is used to screen for inhibition of P-gp by a test compound, by measuring its effect on the bidirectional permeability of a P-gp substrate through Caco-2 cell monolayers.
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This assay is used to identify active uptake of a test compound by PepT1, using the Caco-2 cell monolayer system.
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This assay uses CPT-B1 (BCRP-knockdown), CPT-P1 (P-gp-knockdown), and Caco 2 cell monolayers to determine if a test compound is a substrate and/or inhibitor of BCRP.
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This assay uses CPT-B1 (BCRP-knockdown), CPT-P1 (P-gp-knockdown), and Caco-2 cell monolayers to determine if a test compound is a substrate and/or inhibitor of BCRP.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled human liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled rat liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with liver microsomes in the presence and absence of NADPH.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with S9 fraction in the presence and absence of cofactors.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with either cryopreserved or fresh hepatocytes.
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This assay uses fluorogenic substrates to determine the potency with which a test compound inhibits recombinant human cytochrome P450 (CYP) enzymes.
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This assay is used to screen for inhibition of cytochrome P450 (CYP) enzymes by a test compound.
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Cytochrome P450 reaction phenotyping using CYP-specific Supersomes™
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This assay is used to assess the potential of a test compound to induce CYP1A2, CYP2B6, and CYP3A4 in fresh or cryopreserved human hepatocytes.
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This assay is used to determine the inhibition constant (Ki ) of a test compound and the mechanism of inhibition of CYPs in human liver microsomes (HLM). The IC50 of the test compound for a given CYP must be known or determined with EA407, CYP Inhibition, prior to Ki determination.
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This assay is used to determine the percent remaining and half-life of a test compound incubated with human intestinal microsomes in the presence and absence of NADPH.
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This assay is used to determine the potency with which a test compound inhibits cytochrome P450 (CYP) enzymes.
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This assay is used to determine whether a test compound is a mechanism-based inhibitor of cytochrome P450 (CYP) enzymes.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled mouse liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled primate liver microsomes in the presence of NADPH.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with pooled dog liver microsomes in the presence of NADPH.
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This assay uses fluorogenic substrates to determine the potency with which a test compound inhibits recombinant human cytochrome P450 (CYP) enzymes.
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This assay is used to generate, isolate, and characterize multi-mg quantities of targeted metabolite(s) of a test compound using biomimetic oxidations.
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This assay is used to assess the potential of a test compound to inhibit individual human UDP-glucuronosyltransferase (UGT) isoforms.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with liver S9 fraction (mouse, rat, dog, monkey, or human) in the presence of cofactors.
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This assay is used to determine the percent remaining and intrinsic clearance of a test compound incubated with cryopreserved hepatocytes (mouse, rat, dog, monkey, or human).
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This assay is used to screen for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a single concentration of a test compound.
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This assay is used to determine the IC50 for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a test compound.
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This assay is used to screen for time-dependent inhibition of individual cytochrome P450 (CYP) enzymes by a test compound after pre-incubation with and without NADPH.
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This assay is used to identify time-dependent inhibition of individual cytochrome P450 (CYP) enzymes by a test compound using the IC50 shift approach.
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This assay is used to assess the potential of a test compound to inhibit individual human UDP-glucuronosyltransferase (UGT) isoforms.
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This assay is used to detect glucuronidation of a test compound after incubation with human liver microsomes in the presence of UDPGA.
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This assay is used to detect a glutathione conjugate of a test compound, due to formation of a reactive metabolite, after incubation with human liver microsomes in the presence of NADPH and GSH.
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This assay is used to identify metabolites of a test compound produced by pooled liver microsomes, S9 fraction, or hepatocytes.
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This assay is used to identify and elucidate structures of metabolites of a test compound after incubation with pooled liver microsomes, S9 fraction, or hepatocytes.
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This assay is used to assess the potential of a test compound to induce CYP3A activity in rabbit or dog hepatocytes.
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This assay uses human liver S9 fraction and a chemical inhibitor to determine if a test compound is metabolized by monoamine oxidase (MAO).
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This assay uses fluorogenic substrates to screen for inhibition of recombinant human cytochrome P450 (CYP) enzymes by a single concentration of a test compound.
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This screening assay is used to identify the CYP(s) involved in the metabolism of a test compound, through the use of CYP-specific Supersomes.
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This screening assay is used to identify the CYP(s) involved in the metabolism of a test compound, through the use of human liver microsomes and CYP-specific chemical inhibitors.
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This assay uses recombinant human enzymes (Supersomes) to determine if a test compound is metabolized by flavin-containing monooxygenase (FMO).
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This assay uses recombinant human enzymes (Supersomes) to determine if a test compound is metabolized by monoamine oxidase (MAO).
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This screening assay is used to determine the bioavailability of test compounds relative to a reference compound after oral administration to rats.
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This assay is used to determine the absolute bioavailability of a test compound in mice.
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This assay is used to determine the bioavailability of a test compound in dogs when the compound is administered by at least two different routes.
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This screening assay is used to determine the bioavailability / exposure of test compounds after two routes of administration to male mice.
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This screening assay is used to determine the bioavailability / exposure of test compounds after two routes of administration to male rats.
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This assay is used to determine the bioavailability / exposure of test compounds in male dogs after two routes of administration.
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This assay is used to determine the bioavailability / exposure of a test compound in dogs after two routes of administration (non-crossover).
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This screening assay uses the general CYP inhibitor, 1-aminobenzotriazole (ABT), to determine the role of absorption vs. first-pass metabolism in limiting the systemic exposure of a test compound in rats.
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A quick and cost-effective way to distinguish between poor absorption and rapid first-pass metabolism for compounds with poor oral bioavailability
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A novel way to generate multi-mg quantities of oxidative metabolites
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Structural identification and/or quantification of drug metabolites
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