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T7455

Sigma-Aldrich

Tolvaptan

≥98% (HPLC), powder

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Synonym(s):
N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide, OPC 41061
Empirical Formula (Hill Notation):
C26H25ClN2O3
CAS Number:
Molecular Weight:
448.94
MDL number:
PubChem Substance ID:
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥15 mg/mL

originator

Sanofi Aventis

storage temp.

2-8°C

SMILES string

Cc1ccccc1C(=O)Nc2ccc(c(C)c2)C(=O)N3CCCC(O)c4cc(Cl)ccc34

InChI

1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)

InChI key

GYHCTFXIZSNGJT-UHFFFAOYSA-N

Gene Information

human ... AVPR2(554)

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1 of 4

This Item
O1266SML0204SML0003
vibrant-m

T7455

Tolvaptan

vibrant-m

O1266

OPC 31260 hydrochloride

vibrant-m

SML0204

MS-1020

vibrant-m

SML0003

CID755673

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: ≥15 mg/mL

solubility

DMSO: ≥15 mg/mL

solubility

DMSO: ≥10 mg/mL at 60 °C

solubility

DMSO: ≥15 mg/mL

originator

Sanofi Aventis

originator

-

originator

-

originator

-

Application

Tolvaptan has been used as a V2-selective antagonist for studying its effect on hypertension in mice.

Biochem/physiol Actions

Tolvaptan (OPC 41061) is a potent, orally active non-peptide vasopressin V2 selective antagonist. IC50 = 3 nM at the rat V2 receptor; 29 times more selective for the V2 than for V1a. Tolvaptan has also been shown to inhibit the development of polycystic kidney disease in several animal models.

Features and Benefits

This compound was developed by Sanofi Aventis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Preparation Note

Tolvaptan is soluble in DMSO at a concentration that is greater than or equal to 15 mg/ml.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Nicole K Littlejohn et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 304(10), R818-R828 (2013-03-29)
An indispensable role for the brain renin-angiotensin system (RAS) has been documented in most experimental animal models of hypertension. To identify the specific efferent pathway activated by the brain RAS that mediates hypertension, we examined the hypothesis that elevated arginine
Urine osmolality-guided tolvaptan therapy in decompensated heart failure.
Kaoru Dohi et al.
Circulation journal : official journal of the Japanese Circulation Society, 77(2), 313-314 (2012-12-28)
Teruhiko Imamura et al.
Circulation journal : official journal of the Japanese Circulation Society, 77(2), 397-404 (2012-11-08)
A newly-developed vasopressin type 2 receptor antagonist, tolvaptan (TLV), has a unique feature of diuresis, but the response to this drug can be unpredictable. Data were collected from hospitalized patients with decompensated congestive heart failure who were administered TLV at
Javed Butler et al.
Journal of the American College of Cardiology, 61(5), 571-579 (2012-12-19)
The study investigated whether the number of participants enrolled per site in an acute heart failure trial is associated with participant characteristics and outcomes. Whether and how site enrollment volume affects clinical trials is not known. A total of 4,133
Vicente E Torres et al.
The New England journal of medicine, 367(25), 2407-2418 (2012-11-06)
The course of autosomal dominant polycystic kidney disease (ADPKD) is often associated with pain, hypertension, and kidney failure. Preclinical studies indicated that vasopressin V(2)-receptor antagonists inhibit cyst growth and slow the decline of kidney function. In this phase 3, multicenter

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