UK-157147 |
| Catalog No.GC33809 |
UK-157147 es un sustrato para UDP-glucuronosiltransferasas (UGT1A1) con un valor de Km de 105 μM.
Products are for research use only. Not for human use. We do not sell to patients.
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 | ||
| Formula | C23H24N2O7S | M.Wt | 472.51 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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