A vasopressin V2 receptor antagonist
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Labeled Version(s)
31321Mozavaptan-d6
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Mozavaptan (hydrochloride)

Item No. 16664

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-benzamide, monohydrochloride
CAS Number
138470-70-9
Synonyms
  • OPC 31260
Molecular Formula
C27H29N3O2 • HCl
Formula Weight
464.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 25 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
288 nm
SMILES
CC1=C(C(NC2=CC=C(C(N3C(C=CC=C4)=C4C(N(C)C)CCC3)=O)C=C2)=O)C=CC=C1.Cl
InChi Code
InChI=1S/C27H29N3O2.ClH/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30;/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31);1H
InChi Key
MOROBKPIULFQDC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    50 mg

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    100 mg

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    Product Description

    Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor).1,2 It is selective for vasopressin V2 over V1 receptors (IC50s = 14 and 1,200 nM, respectively) in radioligand binding assays using rat kidney and rat liver membranes that endogenously express high levels of vasopressin V2 and V1 receptors, respectively.1 Mozavaptan (10-30 mg/kg, p.o.) increases urine volume and decreases urine osmolality, indicating aquaresis, in conscious rats. It reduces decreases in urine flow and increases in urine osmolality induced by arginine vasopressin (AVP; Item No. 24154) in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yamamura, Y., Ogawa, H., Yamashita, H., et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br. J. Pharmacol. 105(4), 787-791 (1992).

    2. Nakamura, S., Itoh, S., Fujiki, H., et al. Binding affinities of mozavaptan hydrochloride (OPC-31260) for vasopressin receptors. Jap. Pharmacol. Ther. 34(7), 827-834 (2006).