Home GPCR & G Protein Vasopressin Receptor antagonist Tolvaptan For research use only.

Tolvaptan

Synonyms: OPC-41061

Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.

Tolvaptan Chemical Structure

Tolvaptan Chemical Structure

CAS No. 150683-30-0

Purity & Quality Control

Tolvaptan Related Products

Signaling Pathway

Vasopressin Receptor Signaling Pathways

Vasopressin Receptor Signaling Pathway

Biological Activity

Description Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.
Targets
vasopressin receptor 2 [4]
3 nM
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06171100 Recruiting
Hyponatremia|SIADH
King''s College Hospital NHS Trust
 March 15 2024 --
NCT04182958 Completed
Healthy Adult Male
Otsuka Pharmaceutical Co. Ltd.
 November 25 2019 Phase 1
NCT02994394 Completed
Healthy Adult Male
Otsuka Pharmaceutical Co. Ltd.
 January 6 2017 Phase 1
NCT02729662 Unknown status
Autosomal Dominant Polycystic Kidney Disease
Kyorin University
 October 1 2016 Not Applicable
NCT02020278 Terminated
Hyponatremia
Otsuka Pharmaceutical Development & Commercialization Inc.|Syneos Health
 April 22 2016 Phase 3

Chemical Information & Solubility

Molecular Weight 448.94 Formula

C26H25ClN2O3
CAS No. 150683-30-0 SDF Download Tolvaptan SDF
Smiles CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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