UGT1A1-IN-1
Based on 1 Customer Validation
UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators.
For research use only. We do not sell to patients.
- Purity: 99.27%
- CAS No.: 2097024-37-6
- Formula: C22H19NO3
- Molecular Weight:345.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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UGT1A1 1.33 μM (IC50) |
UGT1A1 5.02 μM (Ki) |
UGT1A1-IN-1 (compound 2) (10-100 μM; 60 min) shows excellent selectivity for recombinant human UGT1A1 over other human UGT isoforms[1].
UGT1A1-IN-1 noncompetitively inhibits UGT1A1-mediated 1-O-glucuronidation in human liver microsomes, with a Ki of 5.02 μM and an IC50 of 1.33 μM[1].
UGT1A1-IN-1 is a high-affinity substrate for recombinant human UGT1A1 (S50 = 0.7 μM) and human liver microsomes (S50 = 4.3 μM), displaying sigmoidal enzymatic kinetics in both systems[1].
UGT1A1-IN-1 (5 μM) acts as a 'turn-on' fluorescent probe for recombinant human UGT1A1, with over 20-fold fluorescence enhancement upon glucuronidation, a linear response to incubation time and enzyme concentration, and a detection limit of 0.48 μg/mL[1].
UGT1A1-IN-1 binds to the same ligand-binding site (site I) on a human UGT1A1 homology model as bilirubin, confirming it can serve as a surrogate for bilirubin in UGT1A1-ligand interaction studies[1].
UGT1A1-IN-1 (5 μM; 30 min) accurately measures UGT1A1 activity in individual human liver microsomes, with activity varying 9-fold across samples and strong correlations with established UGT1A1 probe substrates and protein levels[1].
UGT1A1-IN-1 (5 μM; 30 min) effectively measures UGT1A1 activity in HepG2 cell homogenates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2097024-37-6
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Appearance Solid
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Molecular Weight 345.39
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Formula C22H19NO3
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Color Light yellow to yellow
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SMILES
O=C1C2=CC=CC3=C2C(C(N1CCCC)=O)=CC=C3C4=CC=C(O)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 17.5 mg/mL (50.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8953 mL | 14.4764 mL | 28.9528 mL | 72.3819 mL |
| 5 mM | 0.5791 mL | 2.8953 mL | 5.7906 mL | 14.4764 mL | |
| 10 mM | 0.2895 mL | 1.4476 mL | 2.8953 mL | 7.2382 mL | |
| 15 mM | 0.1930 mL | 0.9651 mL | 1.9302 mL | 4.8255 mL | |
| 20 mM | 0.1448 mL | 0.7238 mL | 1.4476 mL | 3.6191 mL | |
| 25 mM | 0.1158 mL | 0.5791 mL | 1.1581 mL | 2.8953 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9651 mL | 2.4127 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5791 mL | 1.4476 mL |
UGT1A1-IN-1 Related Classifications
HY-160250 Related Classifications
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