In Vitro Metabolism Assay Kits & Reagents

In Vitro Metabolism Assay Kits

The liver is the most important site of drug metabolism. Here the processes of drug inactivation and acquisition of pharmacological activity by the prodrug take place.

Many drugs are metabolized in two phases.

Non-synthetic reactions such as the production of new or modified functional groups or cleavage are included in Phase I reactions (oxidation, reduction, hydrolysis).
Phase II reactions involve synthetic reactions, such as binding to endogenous substances (e.g., glucuronides).

Metabolites formed in synthetic reactions are more polar and therefore more readily excreted by the kidney (urine) and liver (bile) than those formed in non-synthetic reactions. Some drugs undergo only phase I or phase II reactions.

CYP450

In phase I metabolism, the most important enzyme system is cytochrome P-450 (CYP450), a microsomal superfamily of isoenzymes that catalyze the oxidation of many drugs. Electrons are provided by NADPH-CYP450 reductase, a flavoprotein that transfers electrons from NADPH to CYP450.

CYP450 enzymes can be induced or inhibited by many drugs and substances, leading to drug interactions in which one drug enhances the toxicity or reduces the therapeutic effect of another drug.

Glucuronidation

Glucuronidation is the most prevalent phase II reaction and is the only one occurring in the hepatic microsomal enzyme system. Glucuronidation is secreted in the bile and excreted in the urine. Thus, conjugation renders most drugs more soluble and easily excreted by the kidneys. The conjugate produced by binding amino acids to glutamine or glycine is readily excreted in the urine but is not secreted in significant amounts into the bile.

Creative Bioarray provides professional in vitro metabolism assay services and efficient kits, which allows our clients to perform in vitro metabolism testing on their own terms.

In Vitro Metabolism Assay Kits
In Vitro Metabolism Assay Matrix
In Vitro Metabolism Assay Reagents

Related Services

SuperQuick® Cytochrome P450 1A2 (CYP1A2) Activity Assay Kit

Description: CYP1A2 catalyzes the oxidation of polyaromatic hydrocarbons and heterocyclic compounds and is found ...

Cat#: DMK-YS009 INQUIRY

View Product

SuperQuick® Cytochrome P450 1A2 (CYP1A2) Inhibitor Screening Kit

Description: CYP1A2 catalyzes the oxidation of polyaromatic hydrocarbons and heterocyclic compounds and is found ...

Cat#: DMK-YS010 INQUIRY

View Product

SuperQuick® UGT Activity Assay Screening Kit

Description: UGTs are expressed primarily in the liver, intestine, and kidney and catalyze the incorporation of ...

Cat#: DMK-YS011 INQUIRY

View Product

NADPH Regeneration System

Description: NADPH regeneration system serves as a co-factor for drug phase I metabolism reactions, working in ...

Cat#: DMR-M001 INQUIRY

View Product

UGT Incubation System

Description: UGT Incubation System can be directly used for In Vitro drug metabolism assays, eliminating the ...

Cat#: DMR-M002 INQUIRY

View Product