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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Sacubitril sodium (also known as AHU-377), the sodium salt of Sacubitril,is an NEP (neutral endopeptidase 24.11)inhibitor (IC50 = 5 nM) used as a component of the heart failure medicine LCZ696 (LCZ-696; LCZ 696; Entresto; Sacubitril mixture with Valsartan). As a prodrug, Sacubitril has tobe activated to LBQ-657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume.
| ln Vitro |
Brain natriuretic peptide-degrading peptides, including brain natriuretic peptide (BNP), atrial natriuretic peptide (ANP), and natriuretic peptide (NP), are more abundant when sacubitril is present [2].
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| ln Vivo |
Sacubitril (3, 10, and 30 mg/kg, p.o.) pretreatment raised ANP-induced plasma cGMP levels in normotensive rats by 2.4, 3.3, and 4.0 times, respectively (as compared to vehicle, 4 hours AUC) [1]. In Dahl-SS rats, sacubitril sodium (30 and 100 mg/kg, PO) has dose-dependent antihypertensive effects [1].
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| References |
[1]. Hegde, L.G., et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacol 11, P33 (2011).
[2]. Vitiello A, et al. Sacubitril, valsartan and SARS-CoV-2. BMJ Evid Based Med. 2020 Jul 27:bmjebm-2020-111497. [3]. Chrysant SG. Pharmacokinetic, pharmacodynamic, and antihypertensive effects of the neprilysin inhibitor LCZ-696: sacubitril/valsartan. J Am Soc Hypertens. 2017 Jul;11(7):461-468. |
| Molecular Formula |
C24H28NNAO5
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|---|---|
| Molecular Weight |
433.472598075867
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| CAS # |
149690-05-1
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| Related CAS # |
Sacubitril;149709-62-6;Sacubitril hemicalcium salt;1369773-39-6;Sacubitril-d4 hemicalcium salt;Sacubitril-d4;1884269-07-1
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| SMILES |
[Na+].O(CC)C([C@H](C)C[C@@H](CC1C=CC(C2C=CC=CC=2)=CC=1)NC(CCC(=O)[O-])=O)=O
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3070 mL | 11.5348 mL | 23.0696 mL | |
| 5 mM | 0.4614 mL | 2.3070 mL | 4.6139 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3070 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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