Conivaptan HCl(YM 087) - 半岛电竞官方网址

Molecular Weight (MW)	535.04
Formula	C32H26N4O2.HCl
CAS No.	168626-94-6 (HCl)
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility(In vitro)	DMSO: 107 mg/mL (200 mM)
Water: <1 mg/mL
Ethanol: 7 mg/mL (13.1 mM)
Other info	Chemical Name: N-[4-(2-Methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide hydrochloride InChi Key: BTYHAFSDANBVMJ-UHFFFAOYSA-N InChi Code: 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 SMILES Code: O=C(NC1=CC=C(C(N2CCC(NC(C)=N3)=C3C4=CC=CC=C42)=O)C=C1)C5=CC=CC=C5C6=CC=CC=C6.[H]Cl
Synonyms	YM-087 HCl; Conivaptan; Conivaptan; YM 087; YM087; Vaprisol

Molecular Weight (MW)

535.04

Formula

C32H26N4O2.HCl

CAS No.

168626-94-6 (HCl)

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility(In vitro)

DMSO: 107 mg/mL (200 mM)

Water: <1 mg/mL

Ethanol: 7 mg/mL (13.1 mM)

Other info

Chemical Name: N-[4-(2-Methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide hydrochloride
InChi Key: BTYHAFSDANBVMJ-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=C(NC1=CC=C(C(N2CCC(NC(C)=N3)=C3C4=CC=CC=C42)=O)C=C1)C5=CC=CC=C5C6=CC=CC=C6.[H]Cl

Synonyms

YM-087 HCl; Conivaptan; Conivaptan; YM 087; YM087; Vaprisol

In Vitro	In vitroactivity: 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.
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. 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. 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.
Animal model	Rats
Formulation & Dosage	0.03, 0.1 and 0.3 mg/kg i.v.
References	Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51; J Hepatol. 2003 Jun;38(6):755-61.

In Vitro

In vitroactivity: 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.

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. 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. 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.

Animal model

Rats

Formulation & Dosage

0.03, 0.1 and 0.3 mg/kg i.v.

References

Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51; J Hepatol. 2003 Jun;38(6):755-61.

CAS NO:	168626-94-6
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议