168626-94-6
Chemical Structure
Conivaptan hydrochloride
Synonym(s): YM 087
- CAS No.: 168626-94-6
- Formula:C32H27ClN4O2
- Molecular Weight:535.04
IUPAC Name: N-(4-(2-methyl-1,4,5,6-tetrahydrobenzo[b]imidazo[4,5-d]azepine-6-carbonyl)phenyl)-[1,1'-biphenyl]-2-carboxamide hydrochloride
InChIKey: BTYHAFSDANBVMJ-UHFFFAOYSA-N
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
Biological Activity: Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure[1][2].
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Conivaptan hydrochloride | 99.95% | Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure. | ||||||||||||||||||||
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Conivaptan hydrochloride (Standard) | ≥98% | Conivaptan hydrochloride (Standard) (YM 087 (Standard)) is the analytical standard of Conivaptan hydrochloride (HY-18347A). This product is intended for research and analytical applications. Conivaptan hydrochloride is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure. | ||||||||||||||||||||
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References
- [1]. Ali F, et al. Conivaptan: A Dual Receptor Vasopressin V1a/V2 Antagonist. Cardiovascular Drug Reviews, 2007, 25(3): 261-279.
- [2]. Wada K, et al. Effect of the vasopressin receptor antagonist conivaptan in rats with heart failure following myocardial infarction. European journal of pharmacology. 2002 Aug 23;450(2):169-77.
