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Tolvaptan

In stock
Catalog No.
B2300
AVP V2-receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
5mg
$75.00
In stock
25mg
$225.00
In stock
50mg
$330.00
In stock

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Background

Tolvaptan is a selective and oral active antagonist of arginine vasopressin (AVP) V2-receptor with Ki value of 0.43nM [1].

Tolvaptan is a nonpeptide AVP V2-receptor antagonist. It prevents AVP from binding to V2-receptor. In the in vitro binding assay using HeLa cells expressing human AVP receptor subtypes, tolvaptan shows inhibitory activity against V2 and V1a receptors with Ki values of 0.43nM and 12.3nM, respectively. The V1b receptor and 30 other receptors or ion channels are not sensitive to tolvaptan, indicating that tolvaptan is selective to V2-receptor. Tolvaptan also inhibits the production of cAMP induced by AVP with IC50 value of 8nM [1].

In animal models, the tolvaptan induced aquaresis results in increased urine volume and serum sodium. In rat models of acute and chronic hyponatremia, administration of tolvaptan increases plasma sodium levels and decreases the mortality [1].

References:
[1] Miyazaki T, Fujiki H, Yamamura Y, et al. Tolvaptan, an Orally Active Vasopressin V2-Receptor Antagonist-Pharmacology and Clinical Trials. Cardiovascular drug reviews, 2007, 25(1): 1-13.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt448.94
Cas No.150683-30-0
FormulaC26H25ClN2O3
Solubility≥17.8mg/mL in DMSO
Chemical NameN-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
SDFDownload SDF
Canonical SMILESCC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Tolvaptan