product name LCZ696
Description: LCZ696, chemically consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. In Sprague-Dawley rats, oral administration of LCZ696 led to a dose-dependent rise in immunoreactivity of atrial natriuretic peptide resulting from neprilysin inhibition. In hypertensive double transgenic rats, LCZ696 caused a dose-dependent and sustained reduction in mean arterial pressure.
References: J Clin Pharmacol. 2010 Apr;50(4):401-14; Circ Heart Fail. 2015 Jan;8(1):71-8.
915.98
Formula
C24H29N5O3.C24H29NO5.5/2H2O.3Na
CAS No.
936623-90-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 30 mg/mL warmed (32.8 mM)
Water: 100 mg/mL (109.2 mM)
Ethanol: 9 mg/mL (9.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity, LCZ696 (60 mg/kg p.o.) induces a dose-dependent and long-lasting reduction in mean arterial pressure (MAP), and stimulates a rapid and dose-dependent augmentation of plasma ANP immunoreactivity. In rat myocardial infarction (MI) model, LCZ696 (68 mg/kg p.o.) attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. |
| Animal model | |
| Formulation & Dosage | |
| References | J Clin Pharmacol. 2010 Apr;50(4):401-14; Circ Heart Fail. 2015 Jan;8(1):71-8. |
