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Merck
CN

T7455

Tolvaptan

≥98% (HPLC), V2-selective antagonist, powder

别名:

N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide, OPC 41061

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关于此项目

经验公式(希尔记法):
C26H25ClN2O3
化学文摘社编号:
分子量:
448.94
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

Tolvaptan, ≥98% (HPLC), powder

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)

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.
Tolvaptan is a potent, orally active non-peptide vasopressin V2 receptor antagonist.

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

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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)
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
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
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

全球贸易项目编号

货号GTIN
T7455-25MG04061837373152
T7455-5MG04061832868769

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