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:
产品名称
Tolvaptan, ≥98% (HPLC), powder
SMILES string
Cc1ccccc1C(=O)Nc2ccc(c(C)c2)C(=O)N3CCCC(O)c4cc(Cl)ccc34
InChI key
GYHCTFXIZSNGJT-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥15 mg/mL
originator
Sanofi Aventis
storage temp.
2-8°C
Quality Level
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
新产品
此项目有
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
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
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
[Vasopressin antagonist in hyponatremia. Rapid and simple control of serum sodium concentration].
MMW Fortschritte der Medizin, 154(22), 78-79 (2013-01-10)
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