- Catalog No: MBE-0010
- Species: Human
- Source: ExpiSf9™ Cells
- Substrates: NSAIDs/ opioids/anticancer agents or others
- Overview:
- The uridine diphosphate glucuronosyltransferase 2B7 (UGT2B7) enzyme is a pivotal member of the glucuronosyltransferase (UGT) superfamily, which plays a crucial role in the metabolism and elimination of a wide range of compounds, including drugs, hormones, and other endogenous and exogenous substances. As a biology or pharmacology expert, I will elaborate on the significance of UGT2B7 in drug research and development.
Key Functions of UGT2B7
Metabolic Catalysis:
UGT2B7 catalyzes the conjugation of glucuronic acid from uridine diphosphate glucuronic acid (UDPGA) to lipophilic substrates, transforming them into hydrophilic glucuronide conjugates. This process, known as glucuronidation, enhances the excretion of these compounds through urine or bile, facilitating their elimination from the body.
Tissue Localization:
UGT2B7 is predominantly expressed in the liver and intestine, making it a key enzyme in the metabolism and elimination of orally administered drugs. Its high expression in these tissues underscores its importance in the first-pass metabolism of drugs.
- Application in Drug Development:
- Drug Metabolism Prediction and Optimization:
- UGT2B7 plays a significant role in the metabolism of numerous drugs, including non-steroidal anti-inflammatory drugs (NSAIDs), opioids, and anticancer agents. By studying the interaction between UGT2B7 and drug candidates, researchers can gain insights into the metabolic fate of these compounds, informing decisions on drug design, dosing, and administration routes.
- Toxicity Assessment and Mitigation:
- Knowledge of UGT2B7’s involvement in drug metabolism is crucial for predicting the pharmacokinetic properties of drug candidates. This includes factors such as drug clearance, volume of distribution, and elimination half-life, which are essential for determining appropriate dosing regimens.
- High-Throughput Screening Platforms:
- The ability of UGT2B7 to metabolize multiple drugs simultaneously can lead to drug-drug interactions, where one drug can inhibit or induce the activity of UGT2B7, thereby altering the metabolism of co-administered drugs. Understanding these interactions is essential for predicting and managing potential adverse effects.
- In Vitro and In Vivo Models:
- UGT2B7-mediated glucuronidation can affect the efficacy and toxicity of drugs. As such, UGT2B7 recombinant proteins and in vitro assay systems are valuable tools for screening drug candidates and evaluating their metabolic stability and potential for drug-drug interactions.
- Appearance: Lyophilized powder.
- Endotoxin Level: <1.0 EU/μg, determined by LAL method.
- Purity: Greater than 90% as determined by reducing SDS-PAGE.
- Storage & Stability: Stored at -20°C for 2 years. After reconstitution, it is stable at 4°C for 1 week or -20°C for longer. It is recommended to freeze aliquots at -20°C or -80°C for extended storage.
