tolvaptan

Tolvaptan (OPC-41061) is an orally active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of hyponatremia.

Tolvaptan Impurity [1-(4-Amino-2-methylbenzoyl)-7-chloro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-one] is a pharmaceutical intermediate utilized in the synthesis of various active compounds.

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).

DM-4103 is a primary metabolite of Tolvaptan, predominantly metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4103 inhibits the human liver transport proteins NTCP, BSEP, MRP2, MRP3, and MRP4 with IC50 values of 16.3, 4.15, 51.0, 44.6, and 4.26 μM, respectively, and affects bile acid transport. DM-4103 is applicable for research in autosomal dominant polycystic kidney disease (ADPKD).