Tolvaptan

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Cat.No. 5181 - Tolvaptan | C26H25ClN2O3 | CAS No. 150683-30-0
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)
Datasheet
Citations (1)
Literature

Biological Activity

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.

Compound Libraries

Tolvaptan is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.89 100
ethanol 4.49 10

Preparing Stock Solutions

The following data is based on the product molecular weight 448.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kondo et al (1999) 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. 7 1743 PMID: 10482466

Ghali et al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611 PMID: 19644472

Aihara et al (2014) 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. 349 258 PMID: 24570071

Morooka et al (2012) Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 5 484 PMID: 22628529


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Keywords: Tolvaptan potent selective competitive vasopressin receptors antagonists V2 renal cardial protective renoprotective hyponatremia OPC-41061 Vasopressin Receptors

1 Citation for Tolvaptan

Citations are publications that use Tocris products. Selected citations for Tolvaptan include:

Zeynalov et al (2015) Arginine-Vasopressin Receptor Blocker Conivaptan Reduces Brain Edema and Blood-Brain Barrier Disruption after Experimental Stroke in Mice. Mol Cells 10 e0136121 PMID: 26275173


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