product name Tolvaptan
Description: Tolvaptan (also known as OPC-41061) is a selective, competitive, orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, it is used to treat hyponatremia. Tolvaptan is vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).
References: Cardiovasc Drug Rev. 2007 Spring;25(1):1-13; Biochem Pharmacol. 2008 Mar 15;75(6):1322-30.
448.94
Formula
C26H25ClN2O3
CAS No.
150683-30-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 90 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (13.4 mM)
Solubility (In vivo)
Synonyms
OPC-41061
other peoduct :
| In Vitro |
In vitro activity: Tolvaptan 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 vasopressin-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. Kinase Assay: Cell Assay: |
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| In Vivo | Tolvaptan 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 vasopressin (AVP) excretion in rats with heart failure. |
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| Formulation & Dosage | |
| References | Cardiovasc Drug Rev. 2007 Spring;25(1):1-13; Biochem Pharmacol. 2008 Mar 15;75(6):1322-30. |
