- Catalog No: MBE-0012
- Species: Human
- Source: ExpiSf9™ Cells
- Substrates: Testosterone/Bile Acids/estradiol or others
- Overview:
- The UDP-glucuronosyltransferase (UGT) superfamily, comprising numerous isoforms, plays a pivotal role in the biotransformation of various endogenous and exogenous compounds within the human body. Among these, UGT2B17, a member of the UGT2B subfamily, stands out for its unique substrate specificity and metabolic capabilities, making it an intriguing target for drug discovery and development.
Key Characteristics of UGT2B17
UGT2B17 is a phase II metabolic enzyme responsible for catalyzing the conjugation of glucuronic acid from UDP-glucuronic acid (UDPGA) to various substrates, including drugs, toxins, hormones, and other bioactive molecules. This glucuronidation reaction enhances the water solubility and facilitates the elimination of these compounds from the body, primarily through bile and urine. The specificity and efficiency of UGT2B17 in these reactions are crucial determinants of a compound’s pharmacokinetics, efficacy, and potential for toxicity.
- Application in Drug Development:
- Drug Metabolism Prediction and Optimization:
- In the context of drug development, UGT2B17 plays a vital role in modulating the pharmacokinetic properties of drugs. Drugs that are substrates for UGT2B17 undergo rapid glucuronidation, which can significantly impact their half-life, bioavailability, and elimination pathways. This knowledge is crucial for optimizing drug dosing regimens, minimizing adverse drug reactions, and predicting drug-drug interactions.
- Toxicity Assessment and Mitigation:
- By modulating the glucuronidation rate of drugs through formulation strategies or the co-administration of inhibitors or inducers of UGT2B17, researchers can optimize the pharmacokinetics and therapeutic outcomes of drug products.
- High-Throughput Screening Platforms:
- Given that multiple drugs may compete for the same metabolic enzymes, including UGT2B17, understanding its substrate specificity is essential for predicting and mitigating potential drug-drug interactions. This information can guide the design of safer and more effective drug combinations.
- 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.
