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Conivaptan hydrochloride

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Catalog No. T6453Cas No. 168626-94-6
Alias YM 087, Vaprisol, Conivaptan HCl

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

Conivaptan hydrochloride

Conivaptan hydrochloride

🥰Excellent
Purity: 100%
Catalog No. T6453Alias YM 087, Vaprisol, Conivaptan HClCas No. 168626-94-6
Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
Pack SizePriceAvailabilityQuantity
5 mg$37In Stock
10 mg$59In Stock
25 mg$132In Stock
50 mg$238In Stock
100 mg$397In Stock
200 mg$597In Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
Targets&IC50
V1a (rat liver):0.48nM(Ki), V2 (rat kidney):3.04 nM(Ki)
In vivo
Conivaptan administered intravenously at doses of 0.03, 0.1, and 0.3 mg/kg increases urine volume and decreases urine osmolality in a dose-dependent manner in both myocardial infarction and sham-operated rats. In myocardial infarction rats, a dose of 0.3 mg/kg notably lowers right ventricular systolic pressure, left ventricular end-diastolic pressure, reduces lung/body weight ratio, and right atrial pressure, while significantly enhancing dP/dt(max)/left ventricular pressure. Additionally, conivaptan acutely augments urine volume, reduces osmolality, and at study conclusion, cirrhotic rats treated with the V(1a)/V(2)-AVP receptor antagonist exhibit neither hyponatremia nor hypoosmolality. It also normalizes sodium urine volume without impacting creatinine clearance or arterial pressure. At dosages ranging from 0.01 to 0.1 mg/kg i.v., conivaptan demonstrates a dose-dependent diuretic effect in dogs, effectively inhibits vasopressin-induced pressor effects, and at 0.1 mg/kg, substantially blocks vasoconstriction from exogenous vasopressin. Furthermore, at 0.1 mg/kg i.v., it significantly enhances cardiac function in dogs with congestive heart failure as demonstrated by increases in left ventricular dP/dtmax, cardiac output, and stroke volume, alongside significant reductions in left ventricular end-diastolic pressure and total peripheral vascular resistance.
AliasYM 087, Vaprisol, Conivaptan HCl
Chemical Properties
Molecular Weight535.04
FormulaC32H26N4O2·HCl
Cas No.168626-94-6
SmilesCl.Cc1nc-2c(CCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc-23)[nH]1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 7 mg/mL (13.08 mM)
DMSO: 99 mg/mL (185 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8690 mL9.3451 mL18.6902 mL93.4510 mL
5 mM0.3738 mL1.8690 mL3.7380 mL18.6902 mL
10 mM0.1869 mL0.9345 mL1.8690 mL9.3451 mL
DMSO
1mg5mg10mg50mg
20 mM0.0935 mL0.4673 mL0.9345 mL4.6725 mL
50 mM0.0374 mL0.1869 mL0.3738 mL1.8690 mL
100 mM0.0187 mL0.0935 mL0.1869 mL0.9345 mL

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