Conivaptan hydrochloride
CAS No. : 168626-94-6

Conivaptan hydrochloride
Cat. No. : CS-2015
M. Wt. : 535.04
Size Stock Price Quantity Add to Cart Quotation Online
10mg In-stock $96.0
50mg In-stock $288.0
100mg In-stock $480.0
Products are for research use only. Not for human use. We do not sell to patients.

Bulk Inquiry

Collapse
Your information is safe with us. * Required Fields
  Salutation:
  • Dr.
  • Prof.
  • Mr.
  • Ms.
  • Mrs.
  • Miss.
*Country or Region:
  • United States
  • Canada
  • United Kingdom
  • Australia
  • China
  • Germany
  • France
  • Japan
  • Korea South
  • Switzerland
  • ----------------------------------
  • Albania
  • Algeria
  • Argentina
  • Armenia
  • Australia
  • Austria
  • Azerbaijan
  • Bahrain
  • Bangladesh
  • Barbados
  • Belarus
  • Belgium
  • Bolivia
  • Bosnia Herzegovina
  • Brazil
  • Bulgaria
  • Cameroon
  • Canada
  • Chile
  • China
  • Colombia
  • Croatia
  • Cyprus
  • Czech Republic
  • Denmark
  • Ecuador
  • Egypt
  • Estonia
  • Fiji
  • Finland
  • France
  • Georgia
  • Germany
  • Gibraltar
  • Greece
  • Hungary
  • Iceland
  • India
  • Indonesia
  • Iran
  • Iraq
  • Ireland
  • Israel
  • Italy
  • Japan
  • Jordan
  • Kazakhstan
  • Kenya
  • Korea South
  • Kuwait
  • Latvia
  • Lebanon
  • Libya
  • Lithuania
  • Luxembourg
  • Macedonia
  • Malaysia
  • Malta
  • Mexico
  • Moldova
  • Monaco
  • Mongolia
  • Montenegro
  • Morocco
  • Nepal
  • Netherlands
  • New Zealand
  • Nigeria
  • Norway
  • Oman
  • Pakistan
  • Paraguay
  • Peru
  • Philippines
  • Poland
  • Portugal
  • Puerto Rico
  • Qatar
  • Republic of Benin
  • Romania
  • Russia
  • Saudi Arabia
  • Serbia
  • Singapore
  • Slovakia
  • Slovenia
  • South Africa
  • Spain
  • Sri Lanka
  • Suriname
  • Sweden
  • Switzerland
  • Syria
  • Thailand
  • Tunisia
  • Turkey
  • Ukraine
  • United Arab Emirates
  • United Kingdom
  • United States
  • Uruguay
  • Uzbekistan
  • Venezuela
  • Vietnam
  • Zambia
  • Zimbabwe
  • Other Countries
* Applicant name:
* Organization Name:
* Email address:
* Requested quantity:
  • ug
  • g
  • kg
  • t
  • mL
  • L
* Phone number:
  Remarks:
 
Name, 
Organization Name, 
Email address, 
Requested quantity, 
Phone number, 
  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: Conivaptan hydrochloride; YM 087
Cat. No. : CS-2015
CAS No. : 168626-94-6
Formula: C32H27ClN4O2
M. Wt. : 535.04
Solubility: 10 mM in DMSO

Activity:

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].

Protocol:

Animal Administration: Conivaptan is formulated in vehicle composed of 10% ethanol, 30% propylene glycol and 60% distilled water.[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:

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.

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.

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.

  • Select Batch :
    • CS-2015 12196
    • CS-2015 14819
    • CS-2015 10780
Browsing History
Tags:Conivaptan hydrochloride supplier,Conivaptan hydrochloride purchase,Conivaptan hydrochloride manufacturer,Conivaptan hydrochloride sigma,Conivaptan hydrochloride distributor,cost,Conivaptan hydrochloride buy,Conivaptan hydrochloride for sale
Please enter your email address
Organization name: Email:

Submit success