Microsomal Stability Assay at AxisPharm Laboratories

Overview

AxisPharm Laboratories provides comprehensive liver microsomal stability assays to assess the metabolic stability of compounds. Utilizing liver microsomes—extracted from liver cells—this assay is crucial for understanding how drugs are metabolized in the liver. Drug metabolism can significantly impact a compound’s bioavailability, toxicity, and overall effectiveness. By analyzing how a drug transforms within the liver, researchers can gain insights into its potential efficacy and safety profile.

Key Features of the Microsomal Stability Assay

  • Metabolic Stability Assessment: The assay calculates the rate of clearance of a test compound over time during microsomal incubation. This data is essential for evaluating the compound’s intrinsic clearance.
  • Understanding Drug Metabolism: Helps in determining how a drug is metabolized, the formation of metabolites, and its potential impacts on bioavailability and dosing.
  • Improving Drug Candidates: Provides early identification of metabolic properties, enabling clients to refine drug candidates through structure-activity relationships.

Methodology

Liver microsomes, which are derived from the endoplasmic reticulum of liver cells, contain various enzymes crucial for drug metabolism, including cytochrome P450, flavin monooxygenase, carboxylesterase, and epoxy hydrolase. Due to potential variability between batches, it is important to use consistent liver microsome batches for comparative studies throughout a project.

Available Models

AxisPharm Laboratories offers microsomal stability assays using liver microsomes from a range of species, including:

  • Rats
  • Mice
  • Dogs
  • Monkeys
  • Humans

Why Choose AxisPharm?

  • Precision and Reliability: Our assays provide accurate and reliable data on metabolic stability, critical for drug development.
  • Comprehensive Analysis: We offer a wide range of species to ensure relevant and comparative data across different models.
  • Expertise: Our team of experts ensures high-quality analysis and detailed insights to support your drug development process.

Contact Us

For more information or to schedule a microsomal stability assay, please contact AxisPharm Laboratories.

Microsomal Stability Assay Protocol

Compound concentration 10µM
Species of microsomes Rat, mouse, dog, monkey, human
Microsome concentration 0.7mg/mL
Timepoints（min） 0，10, 30, 60
Cofactor NADPH
DMSO final concentration <0.25%
Positive Control Compound Clozapine, Verapamil
NCF60（without NAPDH for 60 min）
Analysis Method LC-MS/MS
Data delivery T1/2， CLint, CLH, ER

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