1. GPCR/G Protein
  2. Vasopressin Receptor
  3. Mozavaptan

Mozavaptan (Synonyms: OPC-31260)

Cat. No.: HY-18346 Purity: 99.89%
Handling Instructions

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.

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Mozavaptan Chemical Structure

Mozavaptan Chemical Structure

CAS No. : 137975-06-5

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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

IC50: 14 nM (Vasopressin V2 receptor); 1.2 μM (Vasopressin V1 receptor)[1]

In Vitro

Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality[1].
Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hydrated conscious rats (300-350 g)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Dose-dependently increased urine flow and decreased urine osmolality.
Molecular Weight

427.54

Formula

C₂₇H₂₉N₃O₂

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.2 mg/mL (14.50 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3390 mL 11.6948 mL 23.3896 mL
5 mM 0.4678 mL 2.3390 mL 4.6779 mL
10 mM 0.2339 mL 1.1695 mL 2.3390 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.89%

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Keywords:

MozavaptanOPC-31260OPC31260OPC 31260Vasopressin ReceptorNonpeptideargininevasopressin-V2diureticAVPbenzazepineSIADHhyponatremiaInhibitorinhibitorinhibit

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Mozavaptan
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