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Merck
CN

T7455

Sigma-Aldrich

Tolvaptan

≥98% (HPLC), 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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About This Item

经验公式(希尔记法):
C26H25ClN2O3
分子量:
448.94
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to tan

溶解性

DMSO: ≥15 mg/mL

创始人

Sanofi Aventis

储存温度

2-8°C

SMILES字符串

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

基因信息

human ... AVPR2(554)

应用

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

生化/生理作用

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.

特点和优势

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

制备说明

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

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Journal of cardiology, 60(6), 462-469 (2012-10-17)
We evaluated the short-term effects of low-dose tolvaptan treatment on hemodynamic parameters in patients with chronic heart failure (HF). We studied 22 patients (69 ± 10 years) with chronic HF and excess fluid retention despite receiving appropriate medical therapy, including
Urine osmolality-guided tolvaptan therapy in decompensated heart failure.
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Circulation journal : official journal of the Japanese Circulation Society, 77(2), 313-314 (2012-12-28)
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Journal of the American College of Cardiology, 61(5), 571-579 (2012-12-19)
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