Tolvaptan

Name: Tolvaptan
Brand: Tocris Bioscience
SKU: 5181

Tocris Bioscience, part of Bio-Techne | Catalog # 5181

Citations (4)

COA / SDS

Potent and selective vasopressin V2 receptor antagonist; renoprotective and orally active

Key Product Details

Description:	Potent and selective vasopressin V₂ receptor antagonist; renoprotective and orally active
Alternative Names:	OPC-41061
Chemical Name:	N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Purity:	≥98% (HPLC)
Molecular Weight:	448.94

View Full Technical Details for Tolvaptan

Technical Data
Citations

Biological Activity for Tolvaptan

Tolvaptan is a potent and selective competitive vasopressin V₂ receptor antagonist (K_i values are 0.06 and 12.3 nM for V₂ and V_1a receptors respectively). Decreases urine osmolality and increases serum sodium concentrations. Delays the onset of end-stage renal disease in a mouse model of polycystic kidney disease. Exhibits myocardial and renal protective effects in hypertensive heart failure rats. Orally active.

Compound Libraries for Tolvaptan

Tolvaptan is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Tolvaptan

M. Wt	448.94
Formula	C₂₆H₂₅ClN₂O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	150683-30-0
PubChem ID	216237
InChi Key	GYHCTFXIZSNGJT-UHFFFAOYSA-N
Smiles	OC1C2=C(C=CC(Cl)=C2)N(C(C3=C(C)C=C(NC(C4=CC=CC=C4C)=O)C=C3)=O)CCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Tolvaptan

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	44.89	100

Preparing Stock Solutions for Tolvaptan

The following data is based on the product molecular weight 448.94.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.23 mL	11.14 mL	22.27 mL
5 mM	0.45 mL	2.23 mL	4.45 mL
10 mM	0.22 mL	1.11 mL	2.23 mL
50 mM	0.04 mL	0.22 mL	0.45 mL

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References for Tolvaptan

References are publications that support the biological activity of the product.

Morooka Chronic administration of oral vasopressin type 2 receptor antagonist tolv. exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 2012 PMID: 22628529
Ghali Tolvaptan. Nat.Rev.Drug Discov. 2009 PMID: 19644472
Aihara Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury. J.Pharmacol.Exp.Ther. 2014 PMID: 24570071
Kondo 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V₂ receptor antagonist. Bioorg.Med.Chem. 1999 PMID: 10482466