The Express Plus ADME assays are screening assays with fixed protocols, useful for identifying promising drug-like leads at an early stage of drug discovery. On this page are listed those in vitroExpress Plus assays that provide information on plasma protein binding, which is a critical determinant of the amount of drug available for distribution into the various body compartments. At the bottom of the page is a list of Assay Data Sheets, each of which summarizes one assay protocol, for our entire portfolio of Express Plus assays. Each of these assays is also available as a Custom assay, meaning that the protocol can be modified with conditions more appropriate for a particular test compound, additional bioanalytical rigor, etc.
| Catalog No. | Description | USD per Compound (1 compound / 3 or more) |
|---|---|---|
| OS021 | Express Plus ADME In Vitro Sales Order and Sample Submittal Form | |
| EA701 | Human Plasma Protein Binding Determined by Equilibrium Dialysis | $575 / $475 |
| EA702 | Rat Plasma Protein Binding Determined by Equilibrium Dialysis |
$575 / $475 |
| EA707 | Fraction Unbound (Rat or Mouse Brain) | $725 / $725 |
| EA708 | Mouse Plasma Protein Binding Determined by Equilibrium Dialysis | $575 / $475 |
| EA709 | Primate Plasma Protein Binding Determined by Equilibrium Dialysis |
$575 / $475 |
| EA710 | Dog Plasma Protein Binding Determined by Equilibrium Dialysis | $575 / $475 |
| EA713 | Blood to Plasma Partitioning in Mice, Rats, or Humans | $670 / $570 |
Why use an Express Plus Assay?
Please note the following:
This assay is used to determine the solubility of a test compound at room temperature in phosphate buffer at pH 7.4.
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This assay is used to determine the LogD of a test compound at pH 7.4 using the shake-flask method.
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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 determine the chemical stability of a test compound in buffer.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in the apical-to-basolateral direction.
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This assay is used to determine the permeability of a test compound through Caco-2 cell monolayers in the apical-to-basolateral and basolateral- to-apical direction.
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This assay is used to determine the blood-brain barrier (BBB) penetration potential of a test compound using MDR1-MDCK cell monolayers.
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This assay is used to determine the P-gp interaction with a test compound using MDR1-MDCK cell monolayers in both the presence and absence of a P-gp inhibitor.
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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 is used to determine the P-gp interaction with a test compound using CellPort™ CPT-B1 BCRP-knockdown cell monolayers in both the presence and the absence of a P-gp inhibitor.
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This assay is used to determine the BCRP interaction with a test compound using CellPort™ CPT-B1 BCRP-knockdown cell monolayers and wild-type Caco-2 cell monolayers.
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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 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 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 before and after pre-incubation with NADPH.
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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 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 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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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to human plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to rat plasma proteins.
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This assay is used to determine the unbound fraction of test compound in a rat brain homogenate via equilibrium dialysis.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to mouse plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to primate plasma proteins.
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Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to dog plasma proteins.
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This assay is used to determine the blood-to-plasma partition coefficient of a test compound in mice, rats, and humans in vitro.
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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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This assay is used to develop dose vehicle(s) for a test compound, as a solution or suspension prior to in vivo pharmacokinetic testing.
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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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In vitro, in situ, and in vivo models to assess brain penetration potential
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Determination of exposure and bioavailability in preclinical species (rodents to primates)
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