- Catalog No: MBE-0009
- Species: Human
- Source: ExpiSf9™ Cells
- Substrates: Etoposide/Irinotecan/Sulfamethoxazole/NSAIDs/Ribavirin or others
- Overview:
- The uridine diphosphate glucuronosyltransferase 1A10 (UGT1A10) enzyme belongs to the family of glucuronosyltransferases (UGTs), which play a pivotal role in the phase II metabolism of drugs and other xenobiotics in humans. This enzyme is particularly important in the context of drug research and development due to its involvement in the glucuronidation process, a key mechanism for the detoxification and elimination of various compounds.
Key Functions of UGT1A10
Glucuronidation Reaction:
UGT1A10 catalyzes the transfer of glucuronic acid from uridine diphosphate glucuronic acid (UDPGA) to various substrates, including drugs, toxins, and endogenous compounds like hormones and bile acids. This process, known as glucuronidation, results in the formation of water-soluble glucuronide conjugates that can be readily excreted through urine or bile, thereby facilitating the elimination of these compounds from the body.
Tissue Distribution:
While UGT enzymes are widely distributed throughout the body, UGT1A10 is predominantly expressed in the intestine, making it a crucial enzyme for the early clearance of drugs and other compounds before they reach the liver. This feature of UGT1A10 is particularly relevant in drug research, as it can significantly impact the bioavailability and pharmacokinetics of orally administered drugs.
- Application in Drug Development:
- Drug Metabolism Prediction and Optimization:
- UGT1A10 plays a significant role in the metabolism of many drugs, particularly those that undergo intestinal first-pass metabolism. By studying the interaction between UGT1A10 and potential drug candidates, researchers can gain insights into the drug’s metabolic fate and potential for intestinal clearance. This information is crucial for optimizing drug design and dosing regimens.
- Toxicity Assessment and Mitigation:
- Understanding the contribution of UGT1A10 to overall drug clearance can help researchers predict the pharmacokinetic properties of a drug candidate. This, in turn, can inform decisions regarding dosing, formulation, and administration routes.
- High-Throughput Screening Platforms:
- Drugs that inhibit or induce UGT1A10 activity can lead to altered metabolism of co-administered drugs, potentially resulting in adverse drug reactions or reduced therapeutic efficacy. Therefore, assessing the potential for drug-drug interactions involving UGT1A10 is an essential step in the drug development process.
- In Vitro and In Vivo Models:
- 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.
