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UGT1A1-IN-1
Catalog No. T87592 Copy Product Info
Purity: 98.93%
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UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity.
UGT1A1-IN-1
Copy Product Info🥰Excellent
Catalog No. T87592
UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity.
Cas No. 2097024-37-6
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| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $126 | - | In Stock | |
| 5 mg | $313 | - | In Stock | |
| 10 mg | $493 | - | In Stock | |
| 25 mg | $987 | - | In Stock | |
| 50 mg | $1,590 | - | In Stock | |
| 100 mg | $2,420 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $345 | - | In Stock |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
Batch Information
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Purity:98.93%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity. |
| Targets&IC50 | UGT1A1:1.33 μM, UGT1A1:5.02 μM(Ki) |
| In vitro | In vitro HLM assays confirm that UGT1A1-IN-1 is a highly specific, non-competitive inhibitor of UGT1A1, with potency independent of substrate concentration. As a fluorescent probe, it generates a significant signal upon glucuronidation, serving as an effective surrogate for bilirubin to monitor UGT1A1 function [1]. |
| Molecular Weight | 345.39 |
| Formula | C22H19NO3 |
| Cas No. | 2097024-37-6 |
| Smiles | O=C1C2=CC=CC=3C(=CC=C(C(=O)N1CCCC)C23)C=4C=CC(O)=CC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 14 mg/mL (40.53 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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