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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

方案

≥98% (HPLC)

表单

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.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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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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