搜索此博客

2018年5月1日星期二

Original: Sacubitril sodium 149690-05-1 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 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.

Name: Sacubitril sodium 
CAS#: 149690-05-1 (sodium) 
Chemical Formula: C24H28NNaO5 
Exact Mass: 
Molecular Weight: 433.4798 
Elemental Analysis: C, 66.50; H, 6.51; N, 3.23; Na, 5.30; O, 18.45

Related CAS #: 1369773-39-6 (hemi-calcium)   149709-62-6 (free acid)   149690-05-1 (sodium)   936623-90-4 (mixture with valsartan)   936623-90-4   137862-53-4  
Synonym: Sacubitril sodium; AHU377; AHU 377; AHU-377; LCZ696.
IUPAC/Chemical Name: sodium 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate
InChi Key: RRTBVEJIZWGATF-JKSHRDEXSA-M
InChi Code: InChI=1S/C24H29NO5.Na/c1-3-30-24(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;/h4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28);/q;+1/p-1/t17-,21+;/m1./s1
SMILES Code: O=C([O-])CCC(N[C@@H](C[C@@H](C)C(OCC)=O)CC1=CC=C(C2=CC=CC=C2)C=C1)=O.[Na+]
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 and water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO or water
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490

REFERENCES
1: Fox H, Bitter T, Horstkotte D, Oldenburg O. Resolution of Cheyne-Stokes Respiration after Treatment of Heart Failure with Sacubitril/Valsartan: A First Case Report. Cardiology. 2017 Feb 9;137(2):96-99. doi: 10.1159/000455118. [Epub ahead of print] PubMed PMID: 28178694.
2: Böhm M, Young R, Jhund PS, Solomon SD, Gong J, Lefkowitz MP, Rizkala AR, Rouleau JL, Shi VC, Swedberg K, Zile MR, Packer M, McMurray JJ. Systolic blood pressure, cardiovascular outcomes and efficacy and safety of sacubitril/valsartan (LCZ696) in patients with chronic heart failure and reduced ejection fraction: results from PARADIGM-HF. Eur Heart J. 2017 Feb 1. doi: 10.1093/eurheartj/ehw570. [Epub ahead of print] PubMed PMID: 28158398.
3: Kaplinsky E. Changing the treatment of heart failure with reduced ejection fraction: clinical use of sacubitril-valsartan combination. J Geriatr Cardiol. 2016 Nov;13(11):914-923. doi: 10.11909/j.issn.1671-5411.2016.11.006. Review. PubMed PMID: 28133468; PubMed Central PMCID: PMC5253408.
4: Williams B, Cockcroft JR, Kario K, Zappe DH, Brunel PC, Wang Q, Guo W. Effects of Sacubitril/Valsartan Versus Olmesartan on Central Hemodynamics in the Elderly With Systolic Hypertension: The PARAMETER Study. Hypertension. 2017 Mar;69(3):411-420. doi: 10.1161/HYPERTENSIONAHA.116.08556. PubMed PMID: 28093466.
5: Lin W, Ji T, Einolf H, Ayalasomayajula S, Lin TH, Hanna I, Heimbach T, Breen C, Jarugula V, He H. Evaluation of Drug-Drug Interaction Potential Between Sacubitril/Valsartan (LCZ696) and Statins Using a Physiologically Based Pharmacokinetic Model. J Pharm Sci. 2017 Jan 13. pii: S0022-3549(17)30010-2. doi: 10.1016/j.xphs.2017.01.007. [Epub ahead of print] PubMed PMID: 28089685.
6: Tyler JM, Teerlink JR. The safety of sacubitril-valsartan for the treatment of chronic heart failure. Expert Opin Drug Saf. 2017 Feb;16(2):257-263. doi: 10.1080/14740338.2017.1279144. PubMed PMID: 28060547.
7: Wang JG, Yukisada K, Sibulo A Jr, Hafeez K, Jia Y, Zhang J. Efficacy and safety of sacubitril/valsartan (LCZ696) add-on to amlodipine in Asian patients with systolic hypertension uncontrolled with amlodipine monotherapy. J Hypertens. 2016 Dec 24. doi: 10.1097/HJH.0000000000001219. [Epub ahead of print] PubMed PMID: 28030431.
8: Tsutsui H, Momomura S, Saito Y, Ito H, Yamamoto K, Ohishi T, Okino N, Guo W. Efficacy and safety of sacubitril/valsartan (LCZ696) in Japanese patients with chronic heart failure and reduced ejection fraction: Rationale for and design of the randomized, double-blind PARALLEL-HF study. J Cardiol. 2016 Dec 23. pii: S0914-5087(16)30309-4. doi: 10.1016/j.jjcc.2016.11.011. [Epub ahead of print] PubMed PMID: 28024961.
9: Khder Y, Shi V, McMurray JJ, Lefkowitz MP. Sacubitril/Valsartan (LCZ696) in Heart Failure. Handb Exp Pharmacol. 2016 Dec 22. doi: 10.1007/164_2016_77. [Epub ahead of print] PubMed PMID: 28004291.
10: Sacubitril/valsartan for chronic heart failure. Aust Prescr. 2016 Dec;39(6):226-227. Review. PubMed PMID: 27990055; PubMed Central PMCID: PMC5155054.
11: Cheng J. Sacubitril/Valsartan (Entresto) for Heart Failure. Am Fam Physician. 2016 Oct 15;94(8):611-612. PubMed PMID: 27929235.
12: Supasyndh O, Sun N, Kario K, Hafeez K, Zhang J. Long-term (52-week) safety and efficacy of Sacubitril/valsartan in Asian patients with hypertension. Hypertens Res. 2016 Nov 17. doi: 10.1038/hr.2016.151. [Epub ahead of print] PubMed PMID: 27853163.
13: Wang TD, Tan RS, Lee HY, Ihm SH, Rhee MY, Tomlinson B, Pal P, Yang F, Hirschhorn E, Prescott MF, Hinder M, Langenickel TH. Effects of Sacubitril/Valsartan (LCZ696) on Natriuresis, Diuresis, Blood Pressures, and NT-proBNP in Salt-Sensitive Hypertension. Hypertension. 2017 Jan;69(1):32-41. PubMed PMID: 27849566.
14: Ezekowitz JA. Hyperkalemia, Sacubitril/Valsartan, and Mineralocorticoid Antagonists in Patients With Heart Failure. JAMA Cardiol. 2017 Jan 1;2(1):86-87. doi: 10.1001/jamacardio.2016.4731. PubMed PMID: 27842180.
15: Desai AS, Vardeny O, Claggett B, McMurray JJ, Packer M, Swedberg K, Rouleau JL, Zile MR, Lefkowitz M, Shi V, Solomon SD. Reduced Risk of Hyperkalemia During Treatment of Heart Failure With Mineralocorticoid Receptor Antagonists by Use of Sacubitril/Valsartan Compared With Enalapril: A Secondary Analysis of the PARADIGM-HF Trial. JAMA Cardiol. 2017 Jan 1;2(1):79-85. doi: 10.1001/jamacardio.2016.4733. PubMed PMID: 27842179.
16: Brandenburg VM, Rocca HB, Marx N. [Sacubitril / Valsartan in patients with diabetes and heart failure]. Dtsch Med Wochenschr. 2016 Oct;141(22):1647-1649. German. PubMed PMID: 27824422.
17: Faber ES, Gavini M, Ramirez R, Sadovsky R. Rhabdomyolysis After Coadministration of Atorvastatin and Sacubitril/Valsartan (Entresto™) in a 63-Year-Old Woman. Drug Saf Case Rep. 2016 Dec;3(1):14. PubMed PMID: 27804100; PubMed Central PMCID: PMC5089965.
18: Kaplinsky E. Sacubitril/valsartan in heart failure: latest evidence and place in therapy. Ther Adv Chronic Dis. 2016 Nov;7(6):278-290. Review. PubMed PMID: 27803793; PubMed Central PMCID: PMC5076745.
19: Ayalasomayajula S, Langenickel TH, Chandra P, Wolfson ED, Albrecht D, Zhou W, Pal P, Rajman I, Sunkara G. Effect of food on the oral bioavailability of the angiotensin receptor - neprilysin inhibitor sacubitril/valsartan (LCZ696) in healthy subjects
. Int J Clin Pharmacol Ther. 2016 Dec;54(12):1012-1018. PubMed PMID: 27719743.
20: Fala L. Entresto (Sacubitril/Valsartan): First-in-Class Angiotensin Receptor Neprilysin Inhibitor FDA Approved for Heart Failure. Am Health Drug Benefits. 2016 Mar;9(Spec Feature):78-82. PubMed PMID: 27668049; PubMed Central PMCID: PMC5013841.