Tolvaptan (C007B-298950)

InformationTolvaptan (OPC-41061) is an orally effective nonpeptide arginineVasotocin V2 receptorantagonist withIC50of 3 nM, used to treat hyponatremia.In vitroTolvaptan blocks the binding of [(3)H]AVP to human V(2) receptors with 29-fold greater selectivity than that for V(1a) receptors, and showed no inhibition of V(1b) receptors. Tolvaptan inhibits not only the binding of [(3)H]AVP but also the AVP-induced production of cyclic AMP in human V(2)-receptor-expressing HeLa cells. Tolvaptan shows marked aquaresis in healthy and diseased animals. Tolvaptan causes a concentration-dependent inhibition of arginine Vasotocin-induced cAMP production with an apparent IC(50) of 0.1 nM in autosomal dominant polycystic kidney disease (ADPKD) cells. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits AVP-induced Cl(-) secretion and decreases in vitro cyst growth of ADPKD cells cultured within a three-dimensional collagen matrix.In vivoTolvaptan improves hyponatremia, resulting in the prevention of death, and improves organ water retention in rat models with acute and chronic hyponatremia. Tolvaptan reduces cardiac preload without unfavorable effects on renal functions, systemic hemodynamics, or circulating neurohormones in dogs with heart failure (HF). Tolvaptan shows a decrease in kidney weight as well as in cyst and fibrosis volume in animal models of human polycystic kidney disease (PKD). Tolvaptan markedly elevates electrolyte-free water clearance (E-CH(2)O) or aquaresis to a positive value and increases urinary Arginine Vasotocin (AVP) excretion in rats with heart failure.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C26H25ClN2O3 Molecular Weight: 448.94