- Catalog No: MBE-0006
- Species: Human
- Source: ExpiSf9™ Cells
- Substrates: Telmisartan/Estrone or others
- Overview:
- UGT1A7, formally known as UDP-Glucuronosyltransferase 1A7, is a member of the UDP-glucuronosyltransferase (UGT) superfamily, a crucial class of enzymes involved in phase II drug metabolism. As a UDP-glucuronosyltransferase, UGT1A7 plays a pivotal role in catalyzing the conjugation of lipophilic substrates with glucuronic acid, thereby enhancing their water solubility and facilitating excretion. This process is essential for the elimination of drugs, xenobiotics, and endogenous compounds from the body.
Key Features of UGT1A7:
Enzymatic Activity: UGT1A7 specifically catalyzes the glucuronidation of various substrates, including but not limited to drugs, environmental toxins, and endogenous compounds such as estrogen metabolites and plant estrogens. This activity contributes significantly to the overall metabolic capacity of the liver and other tissues expressing UGT1A7.
Tissue Distribution: Although UGT1A7 is expressed in multiple tissues, it is particularly abundant in the liver, where it participates in the metabolism of a wide range of compounds.
Genetic Variations: Like other UGT enzymes, UGT1A7 displays genetic variations that can affect its expression levels and enzymatic activity. These variations can have important implications for individual drug response and metabolism.
- Application in Drug Development:
- Drug Metabolism Prediction and Optimization:
- UGT1A7’s critical role in drug metabolism makes it an essential target for predicting the metabolic fate of new drug candidates. By studying the interaction between UGT1A7 and potential drug substrates, researchers can gain insights into the drug’s pharmacokinetics, including its absorption, distribution, metabolism, and excretion (ADME) properties. This information is crucial for optimizing drug dosing regimens and predicting potential drug-drug interactions.
- Toxicity Assessment and Mitigation:
- UGT1A7’s involvement in the detoxification of various compounds, including drugs and toxins, makes it an important factor in toxicity assessment. By evaluating the impact of UGT1A7 on drug metabolism, researchers can identify potential toxicity concerns early in the drug development process and adjust the drug’s structure or dosing regimen accordingly.
- High-Throughput Screening Platforms:
- UGT1A7’s role in the metabolism of multiple drugs makes it a potential contributor to drug-drug interactions. By studying the interactions between UGT1A7 and other drugs, researchers can identify potential inhibitors or inducers of UGT1A7 activity and develop strategies to mitigate their effects. This is particularly important for drugs with a narrow therapeutic index or those that are known to be metabolized by UGT1A7.
- 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.
