LCZ696 (Valsarta + sacubitril)
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MedKoo CAT#: 314266

CAS#: 936623-90-4

Description: LCZ696 is a potent ARNi inhibitor and an investigational drug to treat heart failure. Chemically, LCZ696 is a mixture of valsartan and sacubitril in a 1:1 molar ratio. As of 2014 it is being developed by Novartis. LCZ696 is co-crystallized valsartan and sacubitril, in a one-to-one molar ratio. According to Sci-Finder database, LCZ696 has a formula as (valsartan)(sacubitril)(3Sodium)(5/2 hydrate), or (2 valsartan)(2 sacubitril) (6 Sodium)(5 hydrate), which has results C96H120N12Na6O21. Molecular Weight: 1915.99 . However, according to wikipedia, One LCZ696 complex consists of 6 valsartan anions, 6 sacubitril anions, 18 sodium cations, and 15 molecules of water, resulting in the molecular formula C288H330N36Na18O48·15H2O and a molecular mass of 5748.03 g/mol. The substance is a white powder consisting of thin hexagonal plates. It is stable in solid form as well as in aqueous (watery) solution with a pH of 5 to 7, and has a melting point of about 138 °C (280 °F).(http://en.wikipedia.org/wiki/Valsartan/sacubitril)


Chemical Structure

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LCZ696 (Valsarta + sacubitril)
CAS# 936623-90-4

Theoretical Analysis

MedKoo Cat#: 314266
Name: LCZ696 (Valsarta + sacubitril)
CAS#: 936623-90-4
Chemical Formula: C96H120N12Na6O21
Exact Mass:
Molecular Weight: 1915.99
Elemental Analysis:

Size Price Shipping out time Quantity
100mg USD 150 Same day
200mg USD 250 Same day
500mg USD 650 Same day
1g USD 1150 Same day
2g USD 1950 Same day
5g USD 2950 Same day
10g USD 3950 Same day
50g USD 6950 2 Weeks
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Pricing updated 2021-02-28. Prices are subject to change without notice.

LCZ696, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 936623-90-4   137862-53-4   149690-05-1 (sodium)  

Synonym: LCZ696; LCZ-696; LCZ 696. valsartan / sacubitril (1:1). Brand name: Entresto.

IUPAC/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

InChi Key: UOLUPHRXIRFONO-JOYYXRJNSA-K

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

SMILES Code: 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

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 (100mg/mL) and water (50mg/mL)

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

Preparing Stock Solutions

The following data is based on the product molecular weight 1915.99 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Fabris E, Merlo M, Rapezzi C, Ferrari R, Metra M, Frigerio M, Sinagra G. Sacubitril/Valsartan: Updates and Clinical Evidence for a Disease-Modifying Approach. Drugs. 2019 Sep;79(14):1543-1556. doi: 10.1007/s40265-019-01181-2. Review. PubMed PMID: 31432436.

2: Dewan P, Docherty KF, McMurray JJV. Sacubitril/Valsartan in Asian Patients with Heart Failure with Reduced Ejection Fraction. Korean Circ J. 2019 Jun;49(6):469-484. doi: 10.4070/kcj.2019.0136. Review. PubMed PMID: 31172710; PubMed Central PMCID: PMC6554586.

3: De Vecchis R, Ariano C. Vasodilatory Properties of Sacubitril/Valsartan Explored in Hypertensives Aged Over 55 Years: A Meta-Analysis. High Blood Press Cardiovasc Prev. 2019 Apr 1. doi: 10.1007/s40292-019-00313-9. [Epub ahead of print] Review. PubMed PMID: 30937854.

4: Fonseca C, Brito D, Ferreira J, Franco F, Morais J, Silva Cardoso J; Experts opinion, endorsed by the Working Group on Heart Failure of the Portuguese Society of cardiology. Sacubitril/valsartan: A practical guide. Rev Port Cardiol. 2019 May;38(5):309-313. doi: 10.1016/j.repc.2018.10.008. Epub 2019 Jan 22. Review. English, Portuguese. PubMed PMID: 30679005.

5: Sauer AJ, Cole R, Jensen BC, Pal J, Sharma N, Yehya A, Vader J. Practical guidance on the use of sacubitril/valsartan for heart failure. Heart Fail Rev. 2019 Mar;24(2):167-176. doi: 10.1007/s10741-018-9757-1. Review. PubMed PMID: 30565021; PubMed Central PMCID: PMC6394573.

6: Gori M, D'Elia E, Senni M. Sacubitril/valsartan therapeutic strategy in HFpEF: Clinical insights and perspectives. Int J Cardiol. 2019 Apr 15;281:158-165. doi: 10.1016/j.ijcard.2018.06.060. Epub 2018 Nov 9. Review. PubMed PMID: 30420146.

7: Huet F, Akodad M, Kalmanovitch E, Adda J, Agullo A, Batistella P, Roubille C, Roubille F. Potential Uses of Sacubitril/Valsartan: Need for Data on Efficacy and Safety. Am J Cardiovasc Drugs. 2019 Feb;19(1):1-10. doi: 10.1007/s40256-018-0306-z. Review. PubMed PMID: 30345485.

8: Baliga RR. Sacubitril/Valsartan: The Newest Neurohormonal Blocker for Guideline-Directed Medical Therapy for Heart Failure. Heart Fail Clin. 2018 Oct;14(4):479-491. doi: 10.1016/j.hfc.2018.06.012. Epub 2018 Aug 17. Review. PubMed PMID: 30266357.

9: Dargad RR, Prajapati MR, Dargad RR, Parekh JD. Sacubitril/valsartan: A novel angiotensin receptor-neprilysin inhibitor. Indian Heart J. 2018 Jul;70 Suppl 1:S102-S110. doi: 10.1016/j.ihj.2018.01.002. Epub 2018 Jan 8. Review. PubMed PMID: 30122239; PubMed Central PMCID: PMC6097164.

10: Anderson SL, Marrs JC. Sacubitril/valsartan: evaluation of safety and efficacy as an antihypertensive treatment. Drugs Context. 2018 Aug 6;7:212542. doi: 10.7573/dic.212542. eCollection 2018. Review. PubMed PMID: 30116284; PubMed Central PMCID: PMC6089617.

11: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500875/ PubMed PMID: 29999934.

12: Das BB, Scholl F, Vandale B, Chrisant M. Sacubitril/Valsartan: potential treatment for paediatric heart failure. Cardiol Young. 2018 Sep;28(9):1077-1081. doi: 10.1017/S1047951118001014. Epub 2018 Jul 6. Review. PubMed PMID: 29979147.

13: Nicolas D, Reed M. Sacubitril/Valsartan. 2019 Oct 17. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2019 Jan-. Available from http://www.ncbi.nlm.nih.gov/books/NBK507904/ PubMed PMID: 29939681.

14: Yandrapalli S, Khan MH, Rochlani Y, Aronow WS. Sacubitril/valsartan in cardiovascular disease: evidence to date and place in therapy. Ther Adv Cardiovasc Dis. 2018 Aug;12(8):217-231. doi: 10.1177/1753944718784536. Epub 2018 Jun 19. Review. PubMed PMID: 29921166; PubMed Central PMCID: PMC6041873.

15: Sciatti E, Senni M, Lombardi CM, Gori M, Metra M. Sacubitril/valsartan: from a large clinical trial to clinical practice. J Cardiovasc Med (Hagerstown). 2018 Sep;19(9):473-479. doi: 10.2459/JCM.0000000000000687. Review. PubMed PMID: 29917003.

16: Liu RC. Focused Treatment of Heart Failure with Reduced Ejection Fraction Using Sacubitril/Valsartan. Am J Cardiovasc Drugs. 2018 Dec;18(6):473-482. doi: 10.1007/s40256-018-0280-5. Review. PubMed PMID: 29850980; PubMed Central PMCID: PMC6267534.

17: Joly JM, Desai AS. Sacubitril/Valsartan: From Clinical Trials to Real-world Experience. Curr Treat Options Cardiovasc Med. 2018 Apr 23;20(6):45. doi: 10.1007/s11936-018-0638-7. Review. PubMed PMID: 29687191.

18: Kario K. The Sacubitril/Valsartan, a First-in-Class, Angiotensin Receptor Neprilysin Inhibitor (ARNI): Potential Uses in Hypertension, Heart Failure, and Beyond. Curr Cardiol Rep. 2018 Jan 27;20(1):5. doi: 10.1007/s11886-018-0944-4. Review. PubMed PMID: 29374807.

19: Zaid Iskandar M, Lang CC. Sacubitril and valsartan fixed combination to reduce heart failure events in post-acute myocardial infarction patients. Drugs Today (Barc). 2017 Oct;53(10):545-551. doi: 10.1358/dot.2017.53.10.2722396. Review. PubMed PMID: 29286056.

20: Institute for Quality and Efficiency in Health Care. Sacubitril / Valsartan -- Benefit Assessment According to §35a Social Code Book V [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2016 Mar 30. Available from http://www.ncbi.nlm.nih.gov/books/NBK458434/ PubMed PMID: 29144684.



Additional Information

Valsartan/sacubitril (brand name Entresto, previously known as LCZ696) is a combination drug consisting of two antihypertensives (blood pressure lowering drugs), valsartan and sacubitril, in a 1:1 mixture by molecule count developed by Novartis. The combination is often described as a dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) although the two effects are achieved by two different molecules. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015.