UGT1A1-IN-1

UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1. UGT1A1-IN-1 inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 and a Ki value of 1.33 and 5.02 μM. UGT1A1-IN-1 can bind on UGT1A1 at the same ligand-binding site as Bilirubin (HY-N0323) . UGT1A1-IN-1 displays good reactivity in and human liver microsome (HLM) . UGT1A1-IN-1 can serve as a fluorescent probe substrate for UGT1A1 or study bilirubin metabolism disorders[1].

Product Specifications

CAS Number

[2097024-37-6]

UNSPSC

12352005

Target

UGT

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/ugt1a1-in-1.html

Concentration

10mM

Purity

99.27

Solubility

DMSO : 17.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C2=CC=CC3=C2C(C(N1CCCC)=O)=CC=C3C4=CC=C(O)C=C4

Molecular Formula

C22H19NO3

Molecular Weight

345.39

References & Citations

[1]Lv X, et al. A Practical and High-Affinity Fluorescent Probe for Uridine Diphosphate Glucuronosyltransferase 1A1: A Good Surrogate for Bilirubin. J Med Chem. 2017 Dec 14;60 (23) :9664-9675.