DM-4107

DM-4107 is a major metabolite of Tolvaptan (HY-17000) that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4107 inhibits the ability of human liver transporters NTCP, BSEP, MRP3, MRP4 (IC50 values are 95.6, 119, 61.2, 37.9 μM, respectively) and bile acid transport in SCHH cells. DM-4107 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD) [1][2].

Product Specifications

CAS Number

[1346599-75-4]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

P-glycoprotein

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Metabolic Disease

Smiles

CC1=CC=CC=C1C(NC2=CC(C)=C(C(NC3=C(C(O)CCC(O)=O)C=C(Cl)C=C3)=O)C=C2)=O

Molecular Formula

C26H25ClN2O5

Molecular Weight

480.94

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Wan W L, et al. Synthesis of the major metabolites of Tolvaptan[J]. Chinese Chemical Letters, 2012, 23 (12) : 1343-1346.|[2]Slizgi JR, et al. Inhibition of Human Hepatic Bile Acid Transporters by Tolvaptan and Metabolites: Contributing Factors to Drug-Induced Liver Injury? Toxicol Sci. 2016 Jan;149 (1) :237-50.