Mozavaptan

Catalog No.S2920 Batch:S292001

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Technical Data

Formula

C27H29N3O2

Molecular Weight 427.54 CAS No. 137975-06-5
Solubility (25°C)* In vitro 4-Methylpyridine 23 mg/mL warmed with 50ºC water bath (53.79 mM)
DMSO 1 mg/mL (2.33 mM)
Ethanol 1 mg/mL (2.33 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Mozavaptan (OPC-31260) is a novel competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.
Targets
Vasopressin receptor 2 [2] Vasopressin receptor 1 [2]
14 nM 1.2 μM
In vitro Mozavaptan (OPC-31260) is a nonpeptide, orally effective competitive inhibitor of AVP with a V2:V1 receptor selectivity ratio of 25:1 indicating relative V2 receptor selectivity. [1] Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner. [2]
In vivo Mozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. OPC-31260 dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats. [2]

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    10, 30, 100μg/kg

  • Administration

    i.v.

Selleck's Mozavaptan has been cited by 2 publications

Obestatin ameliorates water retention in chronic heart failure by downregulating renal aquaporin 2 through GPR39, V2R and PPARG signaling [ Life Sci, 2019, 10.1016/j.lfs.2019.05.049] PubMed: 31153818
Obestatin Downregulating Aquaporin 2 Plasma Membrane Distribution Through a Short-Term Regulatory Effect [ Am J Med Sci, 2019, 357(3):247-254] PubMed: 30797506

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.