Conivaptan HCl

Catalog No.S2116 Batch:S211601

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Technical Data

Formula

C32H26N4O2.HCl

Molecular Weight 535.04 CAS No. 168626-94-6
Solubility (25°C)* In vitro DMSO 107 mg/mL (199.98 mM)
Ethanol 7 mg/mL (13.08 mM)
Water Insoluble
* <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 Conivaptan HCl(YM 087) is an orally active, non-peptide, vasopressin V1A and V2 receptor antagonist, used in the treatment of euvolemic and hypervolemic hyponatremia.
Targets
Vasopressin receptor 1 [1] Vasopressin receptor 2 [1]
In vivo

Conivaptan (0.03, 0.1 and 0.3 mg/kg i.v.) dose-dependently increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats. Conivaptan (0.3 mg/kg i.v.) significantly reduces right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight and right atrial pressure in myocardial infarction rats. Conivaptan (0.3 mg/kg i.v.) significantly increases dP/dt(max)/left ventricular pressure in myocardial infarction rats. [1] Conivaptan produces an acute increase in urine volume (UV), a reduction in osmolality (UOsm) and, at the end of the investigation, cirrhotic rats receiving the V(1a)/V(2)-AVP receptor antagonist does not show hyponatremia or hypoosmolality. Conivaptan also normalizes U(Na)V without affecting creatinine clearance and arterial pressure. [2] Conivaptan (0.01 to 0.1 mg/kg i.v.) exerts a dose-dependent diuretic effect in dogs without an increase in the urinary excretion of electrolytes, inhibits the pressor effect of exogenous vasopressin in a dose-dependent manner (0.003 to 0.1 mg/kg i.v.) and, at the highest dose (0.1 mg/kg i.v.), almost completely blocks vasoconstriction caused by exogenous vasopressin. Conivaptan (0.1 mg/kg i.v.) improves cardiac function, as evidenced by significant increases in left ventricular dP/dtmax, cardiac output and stroke volume, and reduces preload and afterload, as evidenced by significant decreases in left ventricular end-diastolic pressure and total peripheral vascular resistance in dogs with congestive heart failure. [3]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Antimicrob Agents Chemother, 2017, AAC.01674-17]

Selleck's Conivaptan HCl has been cited by 4 publications

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Depression compromises antiviral innate immunity via the AVP-AHI1-Tyk2 axis [ Cell Res, 2022, 1-17] PubMed: 35821088
A drug repositioning approach reveals Streptococcus mutans is susceptible to a diverse range of established antimicrobials and non-antibiotics. [Saputo S, et al. Antimicrob Agents Chemother, 2017, AAC.01674-17] PubMed: 29061736
Unveiling some FDA-approved drugs as inhibitors of the store-operated Ca2+ entry pathway. [ Sci Rep, 2017, 7(1):12881] PubMed: 29038464

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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.