Microsomal Stability Assay at AxisPharm Laboratories

The liver microsomal stability assay analysis uses the extracted liver cell microsomes to study the metabolic stability of the compound. Drugs are metabolized in the liver. The drug’s metabolism in the body and whether it forms metabolites are also important parameters in assessing the bioavailability, toxicity, and dosing potential of a compound. Metabolic transformation of a drug in the liver can significantly change its efficacy, which may be harmful to the body.

The microsomal stability assay offers a method to calculate the rate of clearance of a test compound over time in microsomal incubations, and these data are used to evaluate intrinsic clearance.

Data from microsomal stability assay allow clients to identify metabolic properties earlier and focus on improving drug candidates through structure-activity relationships.

Liver microsomes are mainly the endoplasmic reticulum of cells and contain many enzymes involved in drug metabolism, including cytochrome P450, flavin monooxygenase, carboxylesterase and epoxy hydrolase. Because different batches of liver microsomes may have large differences, if you need to strictly compare the liver microsomal stability of the compounds in the entire project, you need to plan and order the same batch of liver microsomes in advance.

AxisPharm offers microsomal stability assay in rats, mice, dogs, monkeys, and humans.

Microsomal Stability Assay Protocol

Compound concentration10µM
Species of microsomesRat, mouse, dog, monkey, human
Microsome concentration0.7mg/mL
Timepoints(min)0,10, 30, 60
CofactorNADPH
DMSO final concentration<0.25%
Positive Control CompoundClozapine, Verapamil
NCF60(without NAPDH for 60 min)
Analysis MethodLC-MS/MS
Data deliveryT1/2, CLint, CLH, ER

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