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Catalog No.S2593 Synonyms: OPC-41061

2 publications

Tolvaptan Chemical Structure

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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Selleck's Tolvaptan has been cited by 2 publications

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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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Biological Activity

Description Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.
vasopressin receptor 2 [4]
3 nM
In vitro

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. [1] 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. [2]

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). [1] 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. [3]


Solubility (25°C)

In vitro DMSO 89 mg/mL (198.24 mM)
Ethanol 6 mg/mL (13.36 mM)
Water Insoluble

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Chemical Information

Molecular Weight 448.94


CAS No. 150683-30-0
Storage powder
in solvent
Synonyms OPC-41061
Smiles CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C

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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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Vasopressin Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID