[CAS NO. 150683-30-0] Tolvaptan

Name: Tolvaptan
Brand: Arctom Scientific
SKU: SLK-S2593

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PRODUCTS SPECIFICATIONS [150683-30-0]

Store

Catalog

SLK-S2593

Brand

Selleck

CAS

150683-30-0

DESCRIPTION [150683-30-0]

Overview

MDL	-
Molecular Weight	448.94
Molecular 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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2275 mL	11.1373 mL	22.2747 mL
5 mM	0.4455 mL	2.2275 mL	4.4549 mL
10 mM	0.2227 mL	1.1137 mL	2.2275 mL
50 mM	0.0445 mL	0.2227 mL	0.4455 mL

Description

Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine antagonist with of 3 nM, used to treat hyponatremia.

Targets

vasopressin receptor 2 ^[4]

3 nM

In vitro

Tolvaptan blocks the binding of [(3)H]AVP to human V(2) receptors with 29-fold greater selectivity than that for V(1a) receptors, and showed no inhibition of V(1b) receptors. Tolvaptan inhibits not only the binding of [(3)H]AVP but also the AVP-induced production of cyclic AMP in human V(2)-receptor-expressing HeLa cells. Tolvaptan shows marked aquaresis in healthy and diseased animals. Tolvaptan causes a concentration-dependent inhibition of arginine vasopressin-induced cAMP production with an apparent IC(50) of 0.1 nM in autosomal dominant polycystic kidney disease (ADPKD) cells. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits AVP-induced Cl(-) secretion and decreases in vitro cyst growth of ADPKD cells cultured within a three-dimensional collagen matrix.

In vivo

Tolvaptan improves hyponatremia, resulting in the prevention of death, and improves organ water retention in rat models with acute and chronic hyponatremia. Tolvaptan reduces cardiac preload without unfavorable effects on renal functions, systemic hemodynamics, or circulating neurohormones in dogs with heart failure (HF). Tolvaptan shows a decrease in kidney weight as well as in cyst and fibrosis volume in animal models of human polycystic kidney disease (PKD). Tolvaptan markedly elevates electrolyte-free water clearance (E-CH(2)O) or aquaresis to a positive value and increases urinary Arginine vasopressin (AVP) excretion in rats with heart failure.

References

[1] Miyazaki T, et al. Cardiovasc Drug Rev, 2007, 25(1), 1-13.
[2] Reif GA, et al. Am J Physiol Renal Physiol, 2011, 301(5), F1005-1013.
[3] Veeraveedu PT, et al. Biochem Pharmacol, 2008, 75(6), 1322-1330.

Synonyms

Benzamide, N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-

1H-1-Benzazepine, benzamide deriv.

N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide

OPC 41061

Tolvaptan

Samsca

1-[4-(2-Methylbenzoylamino)-2-methylbenzoyl]-7-chloro-1,2,3,4-tetrahydrobenzo[b]azepin-5-ol

Jynarque

Jinarc