For research use only.
Catalog No.S2593 Synonyms: OPC-41061
CAS No. 150683-30-0
Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.
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Immunoblots of inner medullas from control and tolvaptan-treated rats. Each lane was loaded with a sample from a different rat. Tolvaptan (2.5 mg/day) or vehicle was infused for 4 days. Loading: aquaporin-2 (AQP2), 15 μg; AQP3, 20 μg; AQP4, 25 μg; and urea transporter UT-A1, 25 μg. Values are normalized band densities covering all bands (means ± SE). *Statistical significance (P < 0.05, t-test).
Am J Physiol Renal Physiol 2014 306(3), F359-66. Tolvaptan purchased from Selleck.
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|Description||Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.|
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. 
|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. |
|In vitro||DMSO||89 mg/mL (198.24 mM)|
|Ethanol||6 mg/mL (13.36 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04182958||Recruiting||Drug: (14C)-OPC-61815||Healthy Adult Male||Otsuka Pharmaceutical Co. Ltd.||December 2019||Phase 1|
|NCT02729662||Active not recruiting||Drug: Tolvaptan||Autosomal Dominant Polycystic Kidney Disease||Kyorin University||October 1 2016||Not Applicable|
|NCT02964273||Active not recruiting||Drug: Tolvaptan|Drug: Matching Placebo||Autosomal Dominant Polycystic Kidney Disease (ADPKD)||Otsuka Pharmaceutical Development & Commercialization Inc.||September 2016||Phase 3|
|NCT02020278||Terminated||Drug: Tolvaptan||Hyponatremia||Otsuka Pharmaceutical Development & Commercialization Inc.|Syneos Health||April 22 2016||Phase 3|
|NCT02925221||Recruiting||--||Autosomal Dominant Polycystic Kidney Disease (ADPKD)||Otsuka Canada Pharmaceutical Inc.||January 2016||--|
|NCT02545101||Completed||--||Hyponatremia|Syndrome of Inappropriate ADH (SIADH) Secretion||Otsuka Pharmaceutical Europe Ltd||November 2015||--|
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