Conivaptan hydrochloride

SKU: orb1300756

Description

Conivaptan hydrochloride is a dual V1A/V2 vasopressin receptor antagonist used to treat euvolemic and hypervolemic hyponatremia. It is a valuable research tool for studying vasopressin signaling pathways in both in vitro binding assays and in vivo models of fluid and electrolyte disorders.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 168626-94-6
• MW: 535.04
• Purity: >99.99% (May vary between batches)
• Formula: C₃₂H₂₆N₄O₂·HCl
• SMILES: Cl.Cc1nc-2c(CCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc-23)[nH]1
• Target: Vasopressin Receptor
• Solubility: DMSO:99 mg/mL (185.03 mM);Ethanol:7 mg/mL (13.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.17 mM)

Bioactivity

• Target IC50:
  V2 receptor (rat kidney):3.04 nM(Ki)|V1a receptor(rat liver):0.48nM(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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Conivaptan, Conivaptan HCl, Conivaptan Hydrochloride, Conivaptan hydrochloride, inhibit, Inhibitor, YM087, YM-087, YM 087, VasopressinReceptor, Vasopressin Receptor, vasopressin receptor 1a, vasopressin receptor 2, Vaprisol

Compound Identifiers

PubChem CID

216322