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细胞分析试剂盒
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中文名称

UGT活性测定/配体筛选试剂盒(荧光法)

英文名字
UGT Activity Assay / Ligand Screening Kit (Fluorometric)
供应商
Biovision
产品货号
K692-100
产品报价
¥询价/100assays
产品说明书
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产品新闻
背景资料
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产品描述
Uridine diphospho-glucuronosyltransferases (UGTs, EC 2.4.1.17) are a superfamily of microsomal membrane-bound glycosyltransferase enzymes. UGTs are responsible for the vast majority of Phase II biotransformation (conjugation) reactions, in which a hydrophilic moiety is attached to small molecule drugs and other xenobiotics to facilitate their rapid excretion from the body. UGTs are predominantly expressed in the liver, intestine and kidneys, where they catalyze the addition of a glucuronic acid moiety from the nucleotide sugar uridine-5’-diphospho-α-D-glucuronic acid (UDPGA) to nucleophilic hydroxyl, sulfhydryl or amino groups of pharmacologically active drugs, Phase I drug metabolites and certain endogenous substrates such as steroid hormones, bile acids and bilirubin. Isozymes of the UGT family have extremely broad, often overlapping substrate specificities and tend to exhibit modest affinity for substrates but high catalytic turnover rates. UGTs also contribute to ‘first-pass’ presystemic drug metabolism, which dramatically reduces the oral bioavailability of a number of drugs. BioVision’s UGT Activity Assay / Ligand Screening Kit 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. The assay utilizes a highly fluorescent UGT substrate with a large Stokes shift (Ex/Em = 415/502 nm) that allows determination of UGT activity by tracking the drop in fluorescence emission as the substrate is converted into a non-fluorescent glucuronide. The multi-isozyme substrate is glucuronidated by virtually all of the pharmacologically-relevant mammalian UGT1A and UGT2B enzymes. UGT specific activity is calculated by comparing the fluorescence loss versus a control reaction performed in the absence of the required cofactor UDPGA. The kit includes the pore-forming peptide antibiotic Alamethicin, which allows the UGT Substrate and UDPGA to rapidly diffuse across lipid membranes to access the UGT active site located in the lumen of microsomes. For verification of modulation of UGT activity by test ligands, diclofenac, a competitive inhibitor of most human and rodent UGT isozymes, is also included. The assay is highly sensitive, simple to perform and high-throughput adaptable. This assay can detect less than 0.1 mU UGT activity in biological samples. The kit contains a complete set of reagents sufficient for performing 100 reactions at a 100 μl reaction volume
产品特点
• Easy-to-use • Non-radioactive • Accurately measure UGT activity in microsomes, lysates and recombinant UGT preparations
保存建议
-20
其他
BioVision的公司总部在美丽的旧金山湾地区,它是全球生命科学公司的领导者.BioVision在开发和研究细胞凋亡检测分析、代谢检测方面具有卓越的影响力.包括检测各种检测分析试剂盒、相关特色抗体、重组蛋白及细胞因子和酶等多种产品,以及其他创新的研究工具.其产品覆盖细胞凋亡研究、能量代谢、细胞/组织蛋白提取、氧化应激与损伤、代谢与肥胖症、细胞增殖与毒性、信号转导、干细胞研究等领域.作为多家知名品牌的中国总代理以及中国区域代理,艾美捷与BioVision一起为研究者们提供最好、最新的细胞生物学研究工具而不断扩大产品及服务质量.
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