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Sacubitrilat (LBQ-657) (Synonyms: Sacubitrilat)

Catalog No.GC30786

Sacubitrilat (LBQ-657) (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

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Sacubitrilat (LBQ-657) Chemical Structure

Cas No.: 149709-44-4

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10mM (in 1mL DMSO)
$119.00
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2mg
$67.00
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5mg
$108.00
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10mg
$180.00
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25mg
$396.00
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50mg
$630.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Sacubitrilat is an active neprilysin (NEP) inhibitor.

Sacubitrilat (LBQ657) is a single diastereomer with specific stereocenters. Sacubitrilat is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency of 5 nM[1].

Pharmacokinetics of Sacubitril, Sacubitrilat (LBQ657), and valsartan following the administration of single oral doses of LCZ696 400 or 1200 mg under fasting condition are summarized. The mean plasma concentrations of Sacubitril increases rapidly with a median Tmax of 0.52 h for the 400 mg dose and 1.05 h for the 1200 mg dose, followed by Sacubitrilat, with the corresponding Tmax values of 2.07 and 3.05 h, respectively. The median Tmax for valsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. The Cmax of Sacubitrilat shows a dose proportional increase, while the Cmax of Sacubitril and Valsartan shows less than proportional increases between the doses. The arithmetic mean AUC0-24 h and AUClast for Sacubitril and Sacubitrilat increases approximately dose proportionally, but shows less than dose proportional increase for Valsartan[2].

[1]. Schiering N, et al. Structure of neprilysin in complex with the active metabolite of sacubitril. Sci Rep. 2016 Jun 15;6:27909. [2]. Langenickel TH, et al. Single therapeutic and supratherapeutic doses of sacubitril/valsartan (LCZ696) do not affect cardiac repolarization. Eur J Clin Pharmacol. 2016 Aug;72(8):917-24.

Chemical Properties

Cas No. 149709-44-4 SDF
Synonyms Sacubitrilat
Canonical SMILES [H]N(C(CCC(O)=O)=O)[C@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@H](C(O)=O)C
Formula C22H25NO5 M.Wt 383.44
Solubility DMSO : ≥ 100 mg/mL (260.80 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.608 mL 13.0398 mL 26.0797 mL
5 mM 0.5216 mL 2.608 mL 5.2159 mL
10 mM 0.2608 mL 1.304 mL 2.608 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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