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Mozavaptan

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Purity:99.26%

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COA HPLC HNMR

Mozavaptan

Catalog No. T6288Cas No. 137975-06-5

Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.

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Pack Size	Price	Availability
10 mg	$48	In Stock
50 mg	$150	In Stock
1 mL x 10 mM (in DMSO)	$55	In Stock

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Product Introduction

Bioactivity

Description	Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.
Targets&IC50	V2 receptor:14 nM, Vasopressin receptor 1:1.2 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]
Kinase Assay	To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis[1].
Alias	OPC31260l, OPC-31260

Chemical Properties

Molecular Weight	427.54
Formula	C27H29N3O2
Cas No.	137975-06-5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 22.5 mg/mL (52.63 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3390 mL	11.6948 mL	23.3896 mL	116.9481 mL
5 mM	0.4678 mL	2.3390 mL	4.6779 mL	23.3896 mL
10 mM	0.2339 mL	1.1695 mL	2.3390 mL	11.6948 mL
20 mM	0.1169 mL	0.5847 mL	1.1695 mL	5.8474 mL
50 mM	0.0468 mL	0.2339 mL	0.4678 mL	2.3390 mL

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