Conivaptan HCl

CAS# 168626-94-6

Conivaptan HCl

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Chemical structure

Conivaptan HCl

3D structure

Chemical Properties of Conivaptan HCl

Cas No. 168626-94-6 SDF Download SDF
PubChem ID 216322 Appearance Powder
Formula C32H27ClN4O2 M.Wt 535.04
Type of Compound N/A Storage Desiccate at -20°C
Synonyms YM 087
Solubility DMSO : ≥ 100 mg/mL (186.90 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide;hydrochloride
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
Standard InChIKey BTYHAFSDANBVMJ-UHFFFAOYSA-N
Standard InChI InChI=1S/C32H26N4O2.ClH/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22;/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Conivaptan HCl

DescriptionConivaptan (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.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].

References:
[1]. Wada K, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51. Epub 2005 Jan 1. [2]. Fernandez-Varo G, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61. [3]. Yatsu T, et al. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46.

Protocol

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.

References:
[1]. Wada K, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51. Epub 2005 Jan 1. [2]. Fernandez-Varo G, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61. [3]. Yatsu T, et al. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46.

Conivaptan HCl Dilution Calculator

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Conivaptan HCl Molarity Calculator

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Preparing Stock Solutions of Conivaptan HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.869 mL 9.3451 mL 18.6902 mL 37.3804 mL 46.7255 mL
5 mM 0.3738 mL 1.869 mL 3.738 mL 7.4761 mL 9.3451 mL
10 mM 0.1869 mL 0.9345 mL 1.869 mL 3.738 mL 4.6725 mL
50 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.7476 mL 0.9345 mL
100 mM 0.0187 mL 0.0935 mL 0.1869 mL 0.3738 mL 0.4673 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Conivaptan HCl

Conivaptan Hydrochloride is a non-peptide inhibitor of antidiuretic hormone. Conivaptan Hydrochloride is used for treatment of congestive heart failure.

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References on Conivaptan HCl

New drugs 07, part I.[Pubmed:17273084]

Nursing. 2007 Feb;37(2):51-8; quiz 59-60.

In this article, you'll learn about 13 new drugs, including: insulin glulisine and insulin detemir, both human insulin analogues; ranolazine, the first drug approved to treat chronic angina in more than a decade; Conivaptan HCl, the first drug approved to treat hyponatremia in patients with normal fluid balance. Unless otherwise specified, the information in the following summaries applies to adults, not children. Consult the package insert for information about each drug's safety during pregnancy and breast-feeding. Also consult the package insert, a pharmacist, or a comprehensive drug reference for more details on precautions, drug interactions, and adverse reactions for all these drugs.

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.

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