1. GPCR/G Protein
  2. Vasopressin Receptor
  3. Conivaptan hydrochloride

Conivaptan hydrochloride (Synonyms: YM 087)

Cat. No.: HY-18347A Purity: 99.92%
Handling Instructions

Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

For research use only. We do not sell to patients.

Conivaptan hydrochloride Chemical Structure

Conivaptan hydrochloride Chemical Structure

CAS No. : 168626-94-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
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10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

IC50 & Target

Ki: 0.48 nM (V1A receptor), 3.04 nM (V2 receptor)

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].

Clinical Trial
Storage

4°C, protect from light

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (186.90 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8690 mL 9.3451 mL 18.6902 mL
5 mM 0.3738 mL 1.8690 mL 3.7380 mL
10 mM 0.1869 mL 0.9345 mL 1.8690 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

At 4 weeks after the operation, 39 myocardial infarction rats survived. Thirty are randomly selected without bias and divided into five groups such that the distribution of infarct size and body weight among groups are similar, and given vehicle, conivaptan (0.03, 0.1 and 0.3 mg/kg) or SR121463A (0.3 mg/kg) by intravenous administration. Sham rats are also divided into four groups and given vehicle or conivaptan (0.03, 0.1 and 0.3 mg/kg) by intravenous administration. Rats are then placed individually in metabolic cages and urine is collected for 3 h. Urine osmolality is measured by the freezing point depression method using an osmometer.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

535.04

Formula

C₃₂H₂₇ClN₄O₂

CAS No.

168626-94-6

SMILES

O=C(C1=CC=CC=C1C2=CC=CC=C2)NC3=CC=C(C(N4CCC(N=C(C)N5)=C5C6=CC=CC=C64)=O)C=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.92%

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Product Name:
Conivaptan hydrochloride
Cat. No.:
HY-18347A
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Conivaptan hydrochloride

Cat. No.: HY-18347A