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Merck

T7455

Tolvaptan

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

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

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About This Item

Empirical Formula (Hill Notation):
C26H25ClN2O3
CAS Number:
150683-30-0
Molecular Weight:
448.94
UNSPSC Code:
51111800
PubChem Substance ID:
329826866
NACRES:
NA.77
MDL number:
MFCD09838782
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Key Documents

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Product Name

Tolvaptan, ≥98% (HPLC), powder

Quality Level

100

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)

Related Categories

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000361457
0000361457
0000135532
0000135532
0000419832

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Mohamed El-Shabrawy et al.
Pharmacology research & perspectives, 8(5), e00659-e00659 (2020-10-01)
Cyclophosphamide (CP) is a chemotherapeutic agent which is extensively used in the treatment of multiple neoplastic and nonneoplastic diseases like breast cancer, lymphomas, systemic lupus erythematosus, and multiple sclerosis. Dose-limiting side effects, mainly nephrotoxicity is a major problem hindering its
Kiyotaka Watanabe et al.
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
Yuya Matsue et al.
Journal of cardiology, 61(2), 169-174 (2012-11-20)
Although tolvaptan is a recently approved drug for heart failure and causes aquaresis without affecting renal function, its clinical efficacy for patients with acute decompensated heart failure (ADHF) is yet to be elucidated. We conducted a prospective observational study in
[Adverse effects of cardiovascular agents in Japan--update 2012].
Yayoi Tetsuou Tsukada
Nihon rinsho. Japanese journal of clinical medicine, 70 Suppl 6, 239-244 (2012-11-20)
Mayuko Ishikawa et al.
International heart journal, 54(2), 98-106 (2013-05-17)
Tolvaptan is a highly selective and orally effective arginine vasopressin V2 receptor antagonist, and is potentially useful for the treatment of heart failure (HF) patients. However, the renoprotective effect of long-term tolvaptan therapy and its underlying mechanisms remain unknown. We
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