Tolvaptan

SKU: orb1305683

Description

Tolvaptan (OPC-41061) is a selective, orally active antagonist of the arginine vasopressin V2 receptor (AVPR2). It is widely used in research to investigate the pathophysiology and treatment of hyponatremia, with applications in both in vitro binding assays and in vivo animal models of water balance disorders.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 150683-30-0
• MW: 448.94
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₂₅ClN₂O₃
• SMILES: C(=O)(N1C=2C(=CC(Cl)=CC2)C(O)CCC1)C3=C(C)C=C(NC(=O)C4=C(C)C=CC=C4)C=C3
• Target: Vasopressin Receptor,Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.14 mM);Ethanol:4.5 mg/mL (10.02 mM);DMSO:240 mg/mL (534.59 mM)

Bioactivity

• Target IC50:
  H69 cells:53.6 μM|NTCP:31.6 μM|HepG2 cells:27.1 µM|V2 receptor (human):0.85 nM (Ki)|V2 receptor (human):1.9 nM|V1 receptor(human):4.9 nM (Ki)|V1 receptor(human):25 nM|MRP2:> 50 μM|BSEP:∼41.5 μM|V2 receptor:3 nM
• In Vivo:
  Tolvaptan demonstrates a concentration-dependent inhibition of arginine vasopressin (AVP)-induced cAMP production in cells affected by Autosomal Dominant Polycystic Kidney Disease (ADPKD), with an IC50 of 0.1 nM. It also suppresses AVP-induced ERK signaling and cell proliferation. Furthermore, Tolvaptan inhibits the secretion of chloride (-) induced by AVP and reduces the extracellular growth of cysts in ADPKD cells cultured in a three-dimensional collagen matrix. It inhibits the binding of [(3)H] AVP to human V(2) receptors with 29 times greater selectivity compared to the V(1a) receptor while showing no inhibitory effect on the V(1b) receptor. In HeLa cells induced by AVP, Tolvaptan inhibits not only the binding of [(3)H] AVP but also the expression of cyclic AMP.
• In Vitro:
  Tolvaptan reduces the pre-cardiac load in dogs with heart failure without adversely affecting renal function, systemic hemodynamics, or circulating neurohormones. In animal models of human polycystic kidney disease, Tolvaptan leads to a reduction in kidney weight and a decrease in cyst fibrosis and volume. Furthermore, Tolvaptan improves hyponatremia and prevents mortality in rat models of acute and chronic hyponatremia. In rats with heart failure, Tolvaptan significantly increases electrolyte-free water clearance (E-CH(2)O) and enhances the excretion of urinary arginine vasopressin.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tolvaptan, SIADH, Vasopressin Receptor, vasopressin receptor 1a, vasopressin receptor 2, VasopressinReceptor, Autophagy, antidiuretic hormone, apoposis, cell cycle, hyponatremia, inhibit, Inhibitor, OPC 41061, OPC41061, OPC-41061

Compound Identifiers

PubChem CID

216237