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T7455

Sigma-Aldrich

Tolvaptan

≥98% (HPLC), 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
MDL number:
MFCD09838782
UNSPSC Code:
51111800
PubChem Substance ID:
329826866
NACRES:
NA.77
Pricing and availability is not currently available.

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[1].

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 Code

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
0000433893
0000433893
0000249171
0000224668
0000224667

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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
[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
Teruhiko Imamura et al.
International heart journal, 54(2), 115-118 (2013-05-17)
Tolvaptan (TLV), a vasopressin type 2 receptor antagonist, has been demonstrated to be effective in patients with decompensated heart failure (HF) refractory to incremental doses of diuretics, but the responsiveness has not always been predictable. We have recently proposed that
Reconsidering chronic hyponatremia in psychosis.
Richard C Josiassen et al.
The Journal of clinical psychiatry, 74(3), 278-279 (2013-04-09)
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