Sacubitrilat
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MedKoo CAT#: 206449

CAS#: 149709-44-4

Description: Sacubitrilat, also known as LBQ657, is endopeptidase inhibitor. Sacubitrilat 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.


Chemical Structure

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Sacubitrilat
CAS# 149709-44-4

Theoretical Analysis

MedKoo Cat#: 206449
Name: Sacubitrilat
CAS#: 149709-44-4
Chemical Formula: C22H25NO5
Exact Mass: 383.17
Molecular Weight: 383.440
Elemental Analysis: C, 68.91; H, 6.57; N, 3.65; O, 20.86

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 400 Ready to ship
100mg USD 650 Ready to ship
250mg USD 1350 Ready to ship
500mg USD 2350 Ready to ship
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Synonym: LBQ-657; LBQ 657; LBQ657; Sacubitrilat

IUPAC/Chemical Name: (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-(3-carboxypropanamido)-2-methylpentanoic acid

InChi Key: DOBNVUFHFMVMDB-BEFAXECRSA-N

InChi Code: InChI=1S/C22H25NO5/c1-15(22(27)28)13-19(23-20(24)11-12-21(25)26)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h2-10,15,19H,11-14H2,1H3,(H,23,24)(H,25,26)(H,27,28)/t15-,19+/m1/s1

SMILES Code: O=C(O)[C@H](C)C[C@H](NC(CCC(O)=O)=O)CC1=CC=C(C2=CC=CC=C2)C=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.
In vitro activity: N/A
In vivo activity: This study demonstrates that neprilysin inhibitor Sac directly improves Ca2+ homeostasis in human end‐stage HF by reducing pro‐arrhythmogenic SR Ca2+ leak without acutely affecting systolic Ca2+ release and inotropy. Reference: ESC Heart Fail. 2020 Oct;7(5):2992-3002. https://pubmed.ncbi.nlm.nih.gov/32710603/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 78.24
DMSO 77.0 200.81
Ethanol 77.0 200.81

Preparing Stock Solutions

The following data is based on the product molecular weight 383.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Eiringhaus J, Wünsche CM, Tirilomis P, Herting J, Bork N, Nikolaev VO, Hasenfuss G, Sossalla S, Fischer TH. Sacubitrilat reduces pro-arrhythmogenic sarcoplasmic reticulum Ca2+ leak in human ventricular cardiomyocytes of patients with end-stage heart failure. ESC Heart Fail. 2020 Oct;7(5):2992-3002. doi: 10.1002/ehf2.12918. Epub 2020 Jul 25. PMID: 32710603; PMCID: PMC7586991.
In vitro protocol: N/A
In vivo protocol: 1. Eiringhaus J, Wünsche CM, Tirilomis P, Herting J, Bork N, Nikolaev VO, Hasenfuss G, Sossalla S, Fischer TH. Sacubitrilat reduces pro-arrhythmogenic sarcoplasmic reticulum Ca2+ leak in human ventricular cardiomyocytes of patients with end-stage heart failure. ESC Heart Fail. 2020 Oct;7(5):2992-3002. doi: 10.1002/ehf2.12918. Epub 2020 Jul 25. PMID: 32710603; PMCID: PMC7586991.

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1: Gan L, Langenickel T, Petruck J, Kode K, Rajman I, Chandra P, Zhou W, Rebello S, Sunkara G. Effects of age and sex on the pharmacokinetics of LCZ696, an angiotensin receptor neprilysin inhibitor. J Clin Pharmacol. 2015 Jun 12. doi: 10.1002/jcph.571. [Epub ahead of print] PubMed PMID: 26073563.

2: Minguet J, Sutton G, Ferrero C, Gomez T, Bramlage P. LCZ696 : a new paradigm for the treatment of heart failure? Expert Opin Pharmacother. 2015 Feb;16(3):435-46. doi: 10.1517/14656566.2015.1000300. Review. PubMed PMID: 25597387.

3: von Lueder TG, Wang BH, Kompa AR, Huang L, Webb R, Jordaan P, Atar D, Krum H. 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. doi: 10.1161/CIRCHEARTFAILURE.114.001785. Epub 2014 Oct 31. PubMed PMID: 25362207.

4: Gu J, Noe A, Chandra P, Al-Fayoumi S, Ligueros-Saylan M, Sarangapani R, Maahs S, Ksander G, Rigel DF, Jeng AY, Lin TH, Zheng W, Dole WP. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14. doi: 10.1177/0091270009343932. Epub 2009 Nov 23. PubMed PMID: 19934029.