Mozavaptan

Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2].

Product Specifications

CAS Number

[137975-06-5]

Product Name Alternative

OPC-31260

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Vasopressin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology; Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Mozavaptan.html

Purity

99.71

Solubility

DMSO : 6.2 mg/mL (warming)

Smiles

CC1=CC=CC=C1C(NC2=CC=C(C(N3C(C=CC=C4)=C4C(N(C)C)CCC3)=O)C=C2)=O

Molecular Formula

C27H29N3O2

Molecular Weight

427.54

Precautions

H302, H315, H319, H335

References & Citations

[1]Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105 (4) :787-91.|[2]Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41 (1) :148-52.