Catalog No.S2593 Synonyms: OPC-41061

Tolvaptan Chemical Structure

Molecular Weight(MW): 448.94

Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.

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In DMSO USD 200 In stock
USD 150 In stock
USD 470 In stock
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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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 448.94


CAS No. 150683-30-0
Storage powder
in solvent
Synonyms OPC-41061

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03048747 Recruiting Syndrome of Inappropriate Antidiuretic Hormone Secretion Otsuka Pharmaceutical Co., Ltd. January 2017 Phase 3
NCT02994394 Recruiting Healthy Adult Male Otsuka Pharmaceutical Co., Ltd. December 2016 Phase 1
NCT02959411 Recruiting Heart Failure|Hyponatremia University of Calgary|Otsuka Canada Pharmaceutical Inc. October 2016 Phase 4
NCT02538016 Not yet recruiting Cystinuria Caleb Nelson|Otsuka America Pharmaceutical|Boston Children’s Hospital October 2016 --
NCT02964273 Recruiting Autosomal Dominant Polycystic Kidney Disease (ADPKD) Otsuka Pharmaceutical Development & Commercialization, Inc. September 2016 Phase 3
NCT02666651 Recruiting Decompensated Heart Failure|Hyponatremia Cardiology Research UBC May 2016 Phase 4

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Vasopressin Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID