UK-157147
目录号 : GC33809
UK-157147是一种UDP-葡萄糖醛酸转移酶(UGT1A1)的底物，Km值为105μM。
Cas No.:162704-20-3
Sample solution is provided at 25 µL, 10mM.
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UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.
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].
[1]. Ethell BT, et al. Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions. Drug Metab Dispos. 2001 Jan;29(1):48-53.
Kinase experiment: | 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]. |
References: [1]. Ethell BT, et al. Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions. Drug Metab Dispos. 2001 Jan;29(1):48-53. | |
| Cas No. | 162704-20-3 | SDF | |
| Canonical SMILES | O=C1C=CC(O[C@H]2[C@](C)(O)C(C)(C)OC3=CC=C(S(=O)(C4=CC=CC(O)=C4)=O)C=C23)=NN1C | ||
| 分子式 | C23H24N2O7S | 分子量 | 472.51 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1164 mL | 10.5818 mL | 21.1636 mL |
| 5 mM | 0.4233 mL | 2.1164 mL | 4.2327 mL |
| 10 mM | 0.2116 mL | 1.0582 mL | 2.1164 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet