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Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $37 | In Stock | |
10 mg | $59 | In Stock | |
25 mg | $132 | In Stock | |
50 mg | $238 | In Stock | |
100 mg | $397 | In Stock | |
200 mg | $597 | In Stock | |
1 mL x 10 mM (in DMSO) | $65 | In Stock |
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. |
Alias | YM 087, Vaprisol, Conivaptan HCl |
Molecular Weight | 535.04 |
Formula | C32H26N4O2·HCl |
Cas No. | 168626-94-6 |
Smiles | Cl.Cc1nc-2c(CCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc-23)[nH]1 |
Relative Density. | no data available |
Storage | Powder: -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
DMSO
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