Tolvaptan
Tocris Bioscience, part of Bio-Techne | Catalog # 5181
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
Product Description
Tolvaptan is a potent and selective competitive vasopressin V2 receptor antagonist (Ki values are 0.06 and 12.3 nM for V2 and V1a 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.Product Specifications
Molecular Weight
448.94
Formula
C26H25ClN2O3
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for Tolvaptan
For research use only
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