tolvaptan

Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.

DM-4111, one of the primary monohydroxy metabolites of Tolvaptan, is an effective vasopressin V2 receptor (vasopressin V2 receptor) inhibitor. By inhibiting water reabsorption in renal tubules, it facilitates the excretion of electrolyte-free water. DM-4111 holds potential for research in cardiovascular diseases.

DM-4107 is a primary metabolite of Tolvaptan, primarily metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4107 inhibits the human liver transport proteins NTCP, BSEP, MRP3, and MRP4, with IC50 values of 95.6, 119, 61.2, and 37.9 μM respectively, affecting bile acid transport. It is applicable for research on autosomal dominant polycystic kidney disease (ADPKD).