2. Metabolic Enzyme/Protease
  3. UGT
  4. UK-157147

UK-157147 是一种 UDP-葡萄糖醛酸转移酶 (UGT1A1) 的底物，Km 值为 105 μM。

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UK-157147 Chemical Structure

UK-157147 Chemical Structure

CAS No. : 162704-20-3

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UK-157147 相关抗体

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  • 生物活性

  • 实验参考方法

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  • 参考文献

生物活性

UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.

IC50 & Target

Km: 105 μM (UGT1A1)[1]
体外研究
(In Vitro)

Glucuronidation is an important pathway for human drug metabolism. Four cloned and expressed human UDP-glucuronosyltransferases (UGT1A1, UGT1A6, UGT1A9, and UGT2B15) are used to screen a series of three potential drug substrates differing only in position of the phenol moiety. The para phenol UK-157147 (UK-157,147) is found to be a substrate for UGT1A1 with a Km value of 105 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

UK-157147 相关抗体:
分子量

472.51

Formula

C23H24N2O7S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Kinase Assay
[1]

UGT assays are performed. Assays are incubated in 100 mM Tris/maleate buffer (pH 7.4) containing 5 mM MgCl2, typically 500 μM substrate, and 350 to 500 μg of cellular sonicate in a total volume of 100 μL. Screening assays are incubated for 60 min at 37°C at two concentrations of UDPGA: 50 μM and 2 mM (containing 0.1 μCi [14C]UDPGA). UDPGA (50 μM) assays allow higher levels of radiolabel incorporation into the glucuronide, which enhances assay sensitivity making this a useful tool for screening. Kinetic determinations are performed at 2 mM UDPGA or higher. The compounds screened are UK-157147 (UK-157,147), UK-156,037, and UK-157,261. Each batch of screening assays is accompanied by positive controls for the cell lines: UGT1A9, 500 μM propofol; UGT1A6, 500 μM 1-naphthol; UGT1A1, 250 μM 17α-ethinylestradiol; and UGT2B15, 500 μM 8-hydroxyquinoline. The unknown compounds are also assayed with human liver microsomes to establish a retention time for the radiolabeled conjugate on the radiochemical HPLC system[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

UK-157147 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UK-157147162704-20-3UK157147UK 157147UGTUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseInhibitorinhibitorinhibit

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产品名称：
UK-157147
目录号：
HY-100319
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