LCZ-696

SKU: orb1223592

Description

A novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio); causes dose-dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawley rats and provides sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats; orally active.Heart Failure Approved(In Vitro):Sacubitril/Valsartan (LCZ696; 1-30 μM; 0.5 hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM).Sacubitril/Valsartan (1-30 μM; 0.5 hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells.(In Vivo):Sacubitril/Valsartan (LCZ696; perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone.

Key Properties

• CAS Number: 936623-90-4
• MW: 957.99
• Purity: >98% (HPLC)
• Formula: C₄₈H₆₀N₆Na₃O₁₀.5
• SMILES: CC(C)[C@@H](C([O-])=O)N(C(CCCC)=O)CC1=CC=C(C2=CC=CC=C2C3=NN=N[N-]3)C=C1.O=C(OCC)[C@H](C)C[C@H](NC(CCC([O-])=O)=O)CC4=CC=C(C5=CC=CC=C5)C=C4.[Na+].[Na+].[Na+].O
• Target: Neprilysin
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Sacubitril/Valsartan (LCZ696; perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone. Animal model: Adult 6-to 8-week-old male Sprague-Dawley rats (220-250 g body weight). Dosage: 68 mg/kg. Administration: Perorally; for 4 weeks. Result: Exhibited small weights and reduced interstitial fibrosis both in the noninfarct zone and peri-infarct zone.
• In Vitro:
  Sacubitril/Valsartan (LCZ696; 1-30 μM; 0.5 hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM). Sacubitril/Valsartan (1-30 μM; 0.5 hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells. Apoptosis Analysis Cell line: HG-treated H9C2 cells. Concentration: 1, 10, or 30 μM. Incubation time: 0.5 hours Result: Inhibited HG-treated H9C2 cells apoptosis. Western blot analysis. Cell line: HG-treated H9C2 cells. Concentration: 1, 10, or 30 μM. Incubation time: 0.5 hours Result: Increased the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LCZ696 | LCZ 696

Quick Database Links

Gene Symbol

Neprilysin