Selective high-performance liquid chromatography-tandem mass spectrometry functional assays of authentic glucuronides for five major hepatic UGT probe substrates were developed: β-estradiol-3-glucuronide (UGT1A1), trifluoperazine-N-glucuronide (UGT1A4), 5-hydroxytryptophol-O-glucuronide (UGT1A6), propofol-O-glucuronide (UGT1A9), and zidovudine ...

UGT-Glo™ Assay (UGT-Glo™ 检测试剂盒 ) 提供了一种利用发光法检测 UDP 葡萄糖醛酸转移酶 (UGT) 活性的方法。 设计 UGT Glo™检测试剂盒是为了检测多种来源的 UGT 活性，比如带有重组表达酶的微粒体或来源于哺乳动物组织的微粒体制备物，还可以测试不同化合物对 UGT 活性的影响。 该检测需要将 UGT 与一个萤光素前体底物共同孵育，一部分底物与 UDP 结合，剩下的底物未被修饰。 随着 D- 半胱氨酸的加入，未经修饰的萤光素前体转变成萤光素，并在一个偶联的 …

We propose a sensitive and reproducible procedure for the activity measurements of four major human hepatic UGT forms. The assays are based on analysis and quantification by high-performance liquid chromatography-tandem mass spectrometry of glucuronides formed from selective probe substrates, namely, beta-estradiol (UGT1A1, 3-glucuronide), 1 ...

Creative Bioarray helps provide CYP and UGT reaction phenotyping assay for CYP1A2, CYP2B6, CYP2C8, CYP3A4, UGT1A1, UGT2B7, or other isoforms on clients' requests. By identifying the enzymes responsible for metabolism, it points out the …

Understand the potential drug-drug interaction liabilities of your compound by using our UGT inhibition assay. UGT inhibition is one of Cyprotex's in vitro experimental ADME services. Cyprotex deliver consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements.

2021年3月8日 · In order to be able to evaluate UGT induction and UGT inhibition, as well as characterize which UGT enzyme(s) are involved in drug metabolism, our team at Den Bosch developed and implemented novel assays to study UGT metabolism for the seven major UGT enzymes (1A1, 1A3, 1A4, 1A6, 1A9, 2B7 and 2B15).

UGT Activity Assay / Ligand Screening Kit (Fluorometric) (ab273331) enables rapid measurement of native or recombinant UGT activity in biological samples such as liver microsomes and can also be used to assess the effect of drugs and other novel compounds on UGT activity.

We present a validated method for the simultaneous evaluation of drug-mediated inhibition of six major UGT isoforms, developed in human liver microsomes through the use of pooled specific UGT probe substrates (cocktail assay) and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis.

In the present study, we examined the selectivity of UGT inhibition with a range of protein concentrations and incubation times in HLM, for a variety of commonly used UGT inhibitors with the goal of identifying selective chemical inhibitors.

2021年4月8日 · Collectively, this study reports a novel fluorescence-based microplate assay for simultaneously sensing the residual activities of ten hUGTs, which strongly facilitates the identification and characterization of UGT inhibitors from drugs or herbal constituents and the investigations on UGT-mediated DDI.