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Express Plus Pharmacokinetics

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 vivo Express Plus assays that provide information on pharmacokinetics and bioavailability in different preclinical species. 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
OS021 Express Plus ADME In Vivo Sales Order and Sample Submittal Form
EA807 Mouse Exposure and/or Bioavailability
  • Individual dosing
  • Cassette dosing: 2-3 compounds
  • Cassette dosing: 4-5 compounds

$5423
$3306
$2759
EA808 Rat Exposure and/or Bioavailability
  • Individual dosing
  • Cassette dosing: 2-3 compounds
  • Cassette dosing: 4-5 compounds

$4455
$2996
$2573
EA810 Dog Exposure and/or Bioavailability
  • One (1) test compound in a single shipment
  • Two (2) or more compounds in a single shipment

$10515
$9915
EA812 Dog Exposure and/or Bioavailability Non-crossover
  • One (1) test compound in a single shipment
  • Two (2) or more compounds in a single shipment

$11215
$10815
EA813 ABT Exposure in Rats $4455
EA982 Formulation Assessment $700

Why use an Express Plus Assay?

  • Because there is no minimum compound requirement and you get significant discounts for multiple compounds
  • Because you get a value added report for a low price
  • Because you will receive your assay results in 10 working days or less
  • Because you get the same well validated test systems for Express Plus assays as you would for our NDA-enabling studies
  • Because you can rely on the quality of our data

Please note the following for in vivo assays:

  • The price for cassette dosing is applicable only if one analytical method and one single injection can be used for the determination of all test compounds.
  • One hour formulation prep cost has been included in the study price. Additional time required for formulation preparation will be charged at $200.00 per hour.
  • The timeline for these studies is ten (10) business days from protocol signoff and test compound receipt, except for the dog exposure assay.
  • The assay results are issued in Basic Report format and delivered via our secure website.

Related Literature

EA104
Express Plus Solubility Assay Data Sheet

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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EA105
Express Plus LogD by Shake-Flask Assay Data Sheet

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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EA153
Express Plus Stability in Plasma or Whole Blood

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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EA154
Express Plus Stability in Buffer

This assay is used to determine the chemical stability of a test compound in buffer.
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EA201
Express Plus Unidirectional Permeability Through Caco-2 Monolayers Assay Data Sheet

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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EA202
Express Plus Bidirectional Permeability Through Caco-2 Monolayers Assay Data Sheet

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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EA203
Express Plus MDR1-MDCK for BBB Penetration Potential Assay Data Sheet

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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EA204
Express Plus P-gp Substrate Assessment Determined Using MDR1-MDCK Cell Monolayers Assay Data Sheet

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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EA222
Express P-gp Inhibitor Assessment Across Cell Monolayers

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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EA224
Express PepT1 Substrate Assessment in Caco-2 Cell Monolayers

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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EA250
Express Plus P-gp Substrate Assessment in CellPort CPT-B1 BCRP Knockdown Cells

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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EA251
Express Plus BCRP Substrate Assessment in CPT-B1 BCRP Knockdown Cells

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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EA401
Express Plus Metabolic Stability (human liver microsomes) Assay Data Sheet

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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EA402
Express Plus Metabolic Stability (rat liver microsomes) Assay Data Sheet

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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EA415
Express Plus Metabolic Stability (mouse liver microsomes) Assay Data Sheet

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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EA416
Express Metabolic Stability (primate liver microsomes) Assay Data Sheet

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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EA417
Express Plus Metabolic Stability (dog liver microsomes) Assay Data Sheet

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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EA418
Express Plus IC50 Determination Using Fluorogenic Substrates

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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EA424
Express Plus Metabolic Stability in Liver S9 Fractions

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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EA425
Express Plus Metabolic Stability in Hepatocytes

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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EA426
Express Plus CYP Inhibition Using LC-MS-MS in Human Liver Microsomes

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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EA427
Express Plus CYP IC50 Using LC-MS-MS in Human Liver Microsomes

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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EA429
Express Plus Time Dependent Inhibition With & without Preincubation

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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EA430
Express Plus Time Dependent Inhibition With & without NADPH

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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EA432
Express Plus UGT Inhibition

This assay is used to assess the potential of a test compound to inhibit individual human UDP-glucuronosyltransferase (UGT) isoforms.
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EA433
Express Plus Detection of Glucuronides

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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EA434
Express Plus Glutathione Trapping

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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EA444
Express Plus CYP Reaction Phenotyping using Supersomes

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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EA445
Express Plus CYP Reaction Phenotyping using Chemical Inhibitors

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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EA701
Express Plus Plasma Protein Binding (human plasma) Assay Data Sheet

Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to human plasma proteins.
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EA702
Express Plus Plasma Protein Binding (rat plasma) Assay Data Sheet

Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to rat plasma proteins.
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EA707
Express Plus Fraction Unbound (rat or mouse brain)

This assay is used to determine the unbound fraction of test compound in a rat brain homogenate via equilibrium dialysis.
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EA708
Express Plus Plasma Protein Binding (mouse plasma) Assay Data Sheet

Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to mouse plasma proteins.
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EA709
Express Plus Plasma Protein Binding (primate plasma) Assay Data Sheet

Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to primate plasma proteins.
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EA710
Express Plus Plasma Protein Binding (dog plasma) Assay Data Sheet

Equilibrium dialysis is used in this assay to determine the percentage of test compound that binds to dog plasma proteins.
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EA713
Express Plus Blood to Plasma Partitioning in Mice Rats and Humans

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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EA807
Express Plus Bioavailability-Exposure in Mice Assay Data Sheet

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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EA808
Express Plus Bioavailability-Exposure in Rats Assay Data Sheet

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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EA810
Express Plus Bioavailability-Exposure in Dogs Assay Data Sheet

This assay is used to determine the bioavailability / exposure of test compounds in male dogs after two routes of administration.
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EA812
Express Plus Bioavailability-Exposure in Dogs Non-crossover

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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EA813
Express Plus ABT Exposure in Rats

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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EA982
Express Plus Formulation Assessment

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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Brochures

ABT Rat Model

A quick and cost-effective way to distinguish between poor absorption and rapid first-pass metabolism for compounds with poor oral bioavailability
Click Here to Download

04/22/10
193 KB
BBB Brain Penetration

In vitro, in situ, and in vivo models to assess brain penetration potential
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10/23/09
1.3 MB
In Vivo Pharmacokinetics

Determination of exposure and bioavailability in preclinical species (rodents to primates)
Click Here to Download

07/20/09
839 KB

References