DC Chemicals Limited
China
Product Name: LBQ-657
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Purity: 98.0%
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Contact: Tony Cao

149709-44-4

149709-44-4 structure

149709-44-4 structure

Name: Sacubitrilat
Chemical Name: (2R,4S)-4-(3-carboxypropanoylamino)-2-methyl-5-(4-phenylphenyl)pentanoic acid
CAS Number: 149709-44-4
Molecular Formula: C₂₂H₂₅NO₅
Molecular Weight: 383.43800
Catalog: Signaling Pathways Metabolic Enzyme/Protease Neprilysin
Create Date: 2016-06-23 10:30:45
Modify Date: 2024-01-02 08:45:29
Sacubitrilat is an active neprilysin (NEP) inhibitor.

Name	(2R,4S)-4-(3-carboxypropanoylamino)-2-methyl-5-(4-phenylphenyl)pentanoic acid
Synonyms	(2R,4S)-5-(Biphenyl-4-yl)-4-((3-carboxypropionyl)amino)-2-methylpentanoic acid LBQ657 UNII-SPI5PBF81S Sacubitrilat

Description	Sacubitrilat is an active neprilysin (NEP) inhibitor.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin Research Areas >> Neurological Disease
Target	Neprilysin[1]
In Vitro	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].
In Vivo	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].
References	[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.

Molecular Formula	C₂₂H₂₅NO₅
Molecular Weight	383.43800
Exact Mass	383.17300
PSA	107.19000
LogP	4.19680
Storage condition	2-8℃