- Catalog No: MBE-0002
- Species: Human
- Source: ExpiSf9™ Cells
- Substrates: Telmisartan/Estrone/2-Hydroxyestrone/Benzopyrene/Quercetin or others
- Overview:
- UGT1A3, formally known as UDP Glucuronosyltransferase 1 Family, Polypeptide A3, is a member of the extensive UGT (Uridine Diphosphate Glucuronosyltransferase) superfamily, which represents one of the most important enzyme families involved in phase II metabolism. UGT1A3 is predominantly localized in the endoplasmic reticulum, microsomes, and membranes, where it exhibits its glucuronidation activity. This enzyme is responsible for catalyzing the conjugation of glucuronic acid, derived from UDP-glucuronic acid (UDPGA), to various lipophilic substrates, including drugs, hormones, and other xenobiotics. The resulting glucuronidated products are generally more water-soluble and can be easily excreted from the body through urine or bile, thereby facilitating detoxification.
- Application in Drug Development:
- Drug Metabolism Prediction and Optimization:
- UGT1A3 plays a significant role in the metabolism of numerous drugs, particularly those with high lipophilicity. By understanding the substrate specificity and kinetic properties of UGT1A3, drug developers can predict the metabolic fate of potential drug candidates, including their clearance rates and potential for drug-drug interactions. This information is crucial for optimizing the pharmacokinetic properties of drugs and ensuring their safety and efficacy
- Toxicity Assessment and Mitigation:
- Drugs that undergo glucuronidation by UGT1A3 may experience altered toxicity profiles depending on individual variations in UGT1A3 expression or activity. Thus, incorporating UGT1A3 into toxicity assessment strategies can help identify potential safety concerns early in the drug development process. This includes evaluating the impact of genetic polymorphisms or environmental factors on UGT1A3 activity and their subsequent effects on drug metabolism and toxicity.
- High-Throughput Screening Platforms:
- As UGT1A3 is involved in the metabolism of multiple drugs, it can be a significant contributor to drug-drug interactions. By studying the interactions between UGT1A3 and other drugs or drug candidates, researchers can identify potential inhibitors or inducers of UGT1A3 activity and assess their impact on drug pharmacokinetics and pharmacodynamics. This information is essential for designing safe and effective drug combination therapies.
- In Vitro and In Vivo Models:
- The development of in vitro and in vivo models that recapitulate human UGT1A3 activity has significantly advanced our understanding of drug-UGT1A3 interactions. These models enable researchers to study the metabolism of drugs in a controlled environment, assess the impact of genetic polymorphisms and environmental factors on UGT1A3 activity, and predict human pharmacokinetic profiles.
- 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.
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