Home GPCR & G Protein Vasopressin Receptor antagonist Conivaptan HCl For research use only.

Conivaptan HCl

Synonyms: YM 087

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.

Conivaptan HCl Chemical Structure

Conivaptan HCl Chemical Structure

CAS: 168626-94-6

Selleck's Conivaptan HCl has been cited by 3 Publications

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Purity & Quality Control

Batch: S211601 DMSO] 107 mg/mL] false] Ethanol] 7 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03000283 Completed Cerebral Hemorrhage|Cerebral Edema|Intracerebral Hemorrhage|Stroke Jesse Corry|Allina Health System March 22 2017 Phase 1
NCT01370148 Completed Liver Disease Cumberland Pharmaceuticals April 2011 Phase 1
NCT00887627 Completed Kidney Diseases|Hyponatremia Cumberland Pharmaceuticals April 2009 Phase 1
NCT00851227 Completed Liver Disease|Hyponatremia Cumberland Pharmaceuticals February 2009 Phase 1

Chemical lnformation & Solubility

Molecular Weight 535.04 Formula

C32H26N4O2.HCl
CAS No. 168626-94-6 SDF Download Conivaptan HCl SDF
Smiles CC1=NC2=C(N1)CCN(C3=CC=CC=C32)C(=O)C4=CC=C(C=C4)NC(=O)C5=CC=CC=C5C6=CC=CC=C6.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 107 mg/mL ( (199.98 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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