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| 10mg |
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| 25mg |
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| 50mg |
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| 250mg |
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Purity: ≥98%
LCZ696 (LCZ-696; LCZ 696; Entresto; Sacubitril mixture with Valsartan), the combination of valsartan with sacubitril in 1:1 molar ratio, is an orally bioavailable and dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) approved in 2015 for the treatment of hypertension and heart failure.
| ln Vitro |
In an experimental model of diabetic cardiomyopathy (DCM), sacubitril/valsartan (LCZ696; 1-30 µM; 0.5 hours) reduces the apoptotic process of HG-treated H9C2 cells[4]. The ratio of Bax/Bcl-2 and the expression level of cleaved caspase-3 are increased in HG-treated H9C2 cells by sacubitril/Valsartan (1-30 µM; 0.5 hours)[4].
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| ln Vivo |
Sacubitril/Valsartan (LCZ696; administered intraperitoneally at a dose of 68 mg/kg for a duration of 4 weeks) considerably diminishes interstitial fibrosis in both the noninfarct and peri-infarct zones[2].
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| Cell Assay |
Apoptosis Analysis[4]
Cell Types: HG-treated H9C2 cells Tested Concentrations: 1, 10, or 30 µM Incubation Duration: 0.5 hrs (hours) Experimental Results: Inhibited HG-treated H9C2 cells apoptosis. Western Blot Analysis[4] Cell Types: HG-treated H9C2 cells Tested Concentrations: 1, 10, or 30 µM Incubation Duration: 0.5 hrs (hours) Experimental Results: Increased the expression level of cleaved caspase- 3 and the ratio of Bax/Bcl-2. |
| Animal Protocol |
Animal/Disease Models: Adult 6- to 8weeks old male SD (Sprague-Dawley) rats (220-250 g body weight) [2]
Doses: 68 mg/kg Route of Administration: Perpo (oral gavage) for 4 weeks Experimental Results: demonstrated small weights and decreased interstitial fibrosis both in the noninfarct zone and peri-infarct zone. |
| References |
[1]. Gu J, et al. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14.
[2]. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. [3]. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. [4]. Ge Q, et al. Feature article: LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates diabeticcardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis. Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039. |
| Molecular Formula |
C48H55N6NA3O8.2.5H2O
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|---|---|
| Molecular Weight |
956.99
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| CAS # |
936623-90-4
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| Related CAS # |
Valsartan;137862-53-4;Valsartan-d9;1089736-73-1
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| 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
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| InChi Key |
UOLUPHRXIRFONO-JOYYXRJNSA-K
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| InChi Code |
InChI=1S/C24H29N5O3.C24H29NO5.3Na.H2O/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23;1-3-30-24(29)17(2)15-21(25-22(26)13-14-23(27)28)16-18-9-11-20(12-10-18)19-7-5-4-6-8-19;;;;/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H2,25,26,27,28,31,32);4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28);;;;1H2/q;;3*+1;/p-3/t22-;17-,21+;;;;/m01..../s1
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| Chemical Name |
sodium (S)-5-(4-((N-(1-carboxylato-2-methylpropyl)pentanamido)methyl)-[1,1-biphenyl]-2-yl)tetrazol-1-ide 4-(((2S,4R)-1-([1,1-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate hydrate
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| Synonyms |
valsartan / sacubitril (1:1); LCZ-696; LCZ696; LCZ 696; trade name: Entresto.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (104.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0449 mL | 5.2247 mL | 10.4494 mL | |
| 5 mM | 0.2090 mL | 1.0449 mL | 2.0899 mL | |
| 10 mM | 0.1045 mL | 0.5225 mL | 1.0449 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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