DM-4103

DM-4103 is a major metabolite of Tolvaptan that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4103 inhibits the ability of human liver transporters NTCP, BSEP, MRP2, MRP3, MRP4 (IC50 values are 16.3, 4.15, 51.0, 44.6, 4.26 μM, respectively) and bile acid transport in SCHH cells. DM-4103 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD)[2].

1346599-56-1

12352005

H302-H315-H319-H335

P-glycoprotein

Membrane Transporter/Ion Channel

Metabolism-protein/nucleotide metabolism

Metabolic Disease

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

C26H23ClN2O5

478.92

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

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W702907/

Reference compound1

No Development Reported