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Metabolism stability refers to the susceptibility of drugs to bio-transformational enzymes such as CYPs and UGTs, which are abundant in the liver. Microsomes from liver are generally used to study in vitro drug metabolism. The metabolism of the drug 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 taking place in liver can change significantly its efficacy, which may be harmful to the body. On this account, drug candidates are tested early in the discovery process for metabolic stability.
The metabolic stability assays offer 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. Microsomal assays primarily assess metabolism by the cytochrome P450 system (phase I enzymes). Data from microsomal assays allow clients to identify metabolic properties earlier and focus on the improvement of drug candidates through structure-activity relationships. We provide microsomal stability assays for all small compounds such as pharmaceuticals, industrial chemicals, and clients’ products.
Microsomal Stability Assay Protocol
|Test system||Human liver microsomes (pooled)|
|Test Compound Concentration||3 µM (or custom)|
|Microsome Concentration||0.5 mg/mL|
|Time Points||0, 5, 15, 30, 45, 60 minutes|
|Number of Replicates||3|
|Negative Control||Vehicle (0.1% DMSO)|
Heat inactivated microsomes
|Positive Controls||Verapamil (rapid clearance)|
Diazepam (low clearance)
|Compound Requirements||50 µL of 10 mM solution|
Creative Bioarray is committed to providing microsomal stability assay service with high effectivity and reliability to accelerate the drug development process. If you have any special needs or questions regarding our services, please feel free to contact us at firstname.lastname@example.org or 1-631-626-9181. We look forward to working with you in the future.
1. Preparation of rat liver microsomes
Rats were sacrificed, and liver was collected and perfused with saline. Liver homogenized using PBS. Liver was homogenized using PBS. The homogenate was centrifuged at 9000 x g for 20 min at 4 °C. Protein concentration was determined and stored at -80 °C until use.
2. Method Validation
As seen in the protocol above, dispense 30 µL of 1.5 µM test compound solution containing 0.5 mg/mL microsomes solution to the assay plates designated for different time points (0, 5, 15, 30, 45 min). After the incubation, transfer the supernatant from each well into a 96-well sample plate for LC/MS analysis.
|Test Article||T1/2 (minute)||CLint (mL/min/kg)||Percent Remaining (%)|
|0 min||5 min||15 min||30 min||45 min|
3. Data Analysis and criteria
Note: K is the rate constant from a plot of ln [concentration] vs. incubation time.
ADME and Pharmacokinetic Services:
In Vitro Metabolism Services: