Sivelestat sodium | neutrophil elastase inhibitor | CAS#150374-95-1

MedKoo Cat#: 128198 | Name: Sivelestat sodium

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Sivelestat sodium (ONO-5046, Sodium sivelestat, LY544349 sodium) is a potent, specific, and intravenously active inhibitor of neutrophil elastase with an IC50 value of 44 nm.

Chemical Structure

Sivelestat sodium

CAS#150374-95-1 (sodium)

Theoretical Analysis

MedKoo Cat#: 128198

Name: Sivelestat sodium

CAS#: 150374-95-1 (sodium)

Chemical Formula: C20H21N2NaO7S

Exact Mass: 456.0967

Molecular Weight: 456.44

Elemental Analysis: C, 52.63; H, 4.64; N, 6.14; Na, 5.04; O, 24.54; S, 7.02

Price and Availability

Size	Price	Availability
5mg	USD 450.00	2 Weeks
25mg	USD 950.00	2 Weeks
100mg	USD 1,650.00	2 Weeks

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Related CAS #

127373-66-4 (free acid) 150374-95-1 (sodium) 201677-61-4 (sodium hydrate)

Synonym

Sivelestat sodium; Sivelestat sodium salt; Sivelestat sodium anhydrous; Sivelestat (sodium)

IUPAC/Chemical Name

sodium (2-((4-(pivaloyloxy)phenyl)sulfonamido)benzoyl)glycinate

InChi Key

ZAIFANJZUGNYCK-UHFFFAOYSA-M

InChi Code

InChI=1S/C20H22N2O7S.Na/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);/q;+1/p-1

SMILES Code

CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)[O-].[Na+]

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 456.44 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.

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

1: Xiao XG, Zu HG, Li QG, Huang P. Sivelestat sodium hydrate attenuates acute lung injury by decreasing systemic inflammation in a rat model of severe burns. Eur Rev Med Pharmacol Sci. 2016 Feb;20(3):528-36. PubMed PMID: 26914130. 2: Wang J, Dai XJ, Zhang YF, Zhong DF, Wu YL, Chen XY. [Simultaneous determination of sivelestat and its metabolite XW-IMP-A in human plasma using HPLC-MS/MS]. Yao Xue Xue Bao. 2015 Oct;50(10):1318-23. Chinese. PubMed PMID: 26837180. 3: Yamada K, Kobayashi H, Bo R, Takahashi T, Hasegawa Y, Nakamura M, Ishige N, Yamaguchi S. Elevation of pivaloylcarnitine by sivelestat sodium in two children. Mol Genet Metab. 2015 Nov;116(3):192-4. doi: 10.1016/j.ymgme.2015.09.009. Epub 2015 Sep 26. PubMed PMID: 26428892. 4: Miyoshi S, Ito R, Katayama H, Dote K, Aibiki M, Hamada H, Okura T, Higaki J. Combination therapy with sivelestat and recombinant human soluble thrombomodulin for ARDS and DIC patients. Drug Des Devel Ther. 2014 Sep 2;8:1211-9. doi: 10.2147/DDDT.S68030. eCollection 2014. PubMed PMID: 25214765; PubMed Central PMCID: PMC4159222. 5: Aikawa N, Kawasaki Y. Clinical utility of the neutrophil elastase inhibitor sivelestat for the treatment of acute respiratory distress syndrome. Ther Clin Risk Manag. 2014 Aug 5;10:621-9. doi: 10.2147/TCRM.S65066. eCollection 2014. Review. PubMed PMID: 25120368; PubMed Central PMCID: PMC4130327. 6: Wang Y, Yang H, Hu Q, Hou Y, Luo H, Liu L. [Effects of sivelestat on acute lung injury in dogs with severe burn-blast combined injury]. Zhonghua Shao Shang Za Zhi. 2014 Apr;30(2):158-65. Chinese. PubMed PMID: 24989662. 7: Wang H, Wang S, Tang A, Gong H, Ma P, Chen L. Combined effects of sivelestat and resveratrol on severe acute pancreatitis-associated lung injury in rats. Exp Lung Res. 2014 Aug;40(6):288-97. doi: 10.3109/01902148.2014.908249. Epub 2014 May 2. PubMed PMID: 24785170. 8: Kohira S, Oka N, Inoue N, Itatani K, Kitamura T, Horai T, Oshima H, Tojo K, Yoshitake S, Miyaji K. Effect of additional preoperative administration of the neutrophil elastase inhibitor sivelestat on perioperative inflammatory response after pediatric heart surgery with cardiopulmonary bypass. Artif Organs. 2014 Dec;38(12):1018-23. doi: 10.1111/aor.12311. Epub 2014 Apr 21. PubMed PMID: 24750107. 9: Yuan Q, Jiang YW, Fang QH. Improving effect of Sivelestat on lipopolysaccharide-induced lung injury in rats. APMIS. 2014 Sep;122(9):810-7. doi: 10.1111/apm.12222. Epub 2014 Feb 1. PubMed PMID: 24484066. 10: Sakai S, Tajima H, Miyashita T, Nakanuma S, Makino I, Hayashi H, Nakagawara H, Kitagawa H, Fushida S, Fujimura T, Saito H, Munesue S, Yamamoto Y, Ohta T. Sivelestat sodium hydrate inhibits neutrophil migration to the vessel wall and suppresses hepatic ischemia-reperfusion injury. Dig Dis Sci. 2014 Apr;59(4):787-94. doi: 10.1007/s10620-013-2963-8. Epub 2013 Dec 8. PubMed PMID: 24318803. 11: Park JS, Park KH, Kim H, Choi SY. Effects of sivelestat treatment on acute lung injury in paraquat-intoxicated rats. Drug Chem Toxicol. 2014 Jan;37(1):114-20. doi: 10.3109/01480545.2013.834351. Epub 2013 Oct 11. PubMed PMID: 24111663. 12: Nomura N, Asano M, Saito T, Nakayama T, Mishima A. Sivelestat attenuates lung injury in surgery for congenital heart disease with pulmonary hypertension. Ann Thorac Surg. 2013 Dec;96(6):2184-91. doi: 10.1016/j.athoracsur.2013.07.017. Epub 2013 Sep 25. PubMed PMID: 24075485. 13: Kumagai K, Saikawa Y, Takeuchi H, Suda K, Fukuda K, Nakamura R, Takahashi T, Kawakubo H, Wada N, Miyasho T, Kitagawa Y. The neutrophil elastase inhibitor sivelestat suppresses accelerated gastrointestinal tumor growth via peritonitis after cecal ligation and puncture. Anticancer Res. 2013 Sep;33(9):3653-9. PubMed PMID: 24023292. 14: Matsuzaki K, Okumi M, Kishimoto N, Yazawa K, Miyagawa Y, Uchida K, Nonomura N. [A case of bladder cancer producing granulocyte colony-stimulating factor and interleukin-6 causing respiratory failure treated with neoadjuvant systemic chemotherapy along with sivelestat]. Hinyokika Kiyo. 2013 Jul;59(7):443-7. Japanese. PubMed PMID: 23945326. 15: Wang H, Tang AM, Liu D, Li G, Ye L, Li X, Li C, Chen L. Renoprotective activity of sivelestat in severe acute pancreatitis in rats. Exp Ther Med. 2013 Jul;6(1):29-32. Epub 2013 Apr 24. PubMed PMID: 23935713; PubMed Central PMCID: PMC3735895. 16: Eguchi T, Yoshida K, Kondo R, Hamanaka K, Shiina T, Komatsu Y, Yamamoto H, Kubo K, Hasegawa J, Koizumi T. Sivelestat prevents cytoskeletal rearrangements in neutrophils resulting from lung re-expansion following one-lung ventilation during thoracic surgery. Inflammation. 2013 Dec;36(6):1479-84. doi: 10.1007/s10753-013-9689-9. PubMed PMID: 23872720. 17: Kohira S, Oka N, Inoue N, Itatani K, Hanayama N, Kitamura T, Fujii M, Takeda A, Oshima H, Tojo K, Yoshitake S, Miyaji K. Effect of the neutrophil elastase inhibitor sivelestat on perioperative inflammatory response after pediatric heart surgery with cardiopulmonary bypass: a prospective randomized study. Artif Organs. 2013 Dec;37(12):1027-33. doi: 10.1111/aor.12103. Epub 2013 Jul 3. PubMed PMID: 23834653. 18: Cao J, Liu Q. Protective effects of sivelestat in a caerulein-induced rat acute pancreatitis model. Inflammation. 2013 Dec;36(6):1348-56. doi: 10.1007/s10753-013-9674-3. PubMed PMID: 23794035. 19: Inoue N, Oka N, Kitamura T, Shibata K, Itatani K, Tomoyasu T, Miyaji K. Neutrophil elastase inhibitor sivelestat attenuates perioperative inflammatory response in pediatric heart surgery with cardiopulmonary bypass. Int Heart J. 2013;54(3):149-53. PubMed PMID: 23774238. 20: Aune SE, Yeh ST, Kuppusamy P, Kuppusamy ML, Khan M, Angelos MG. Sivelestat attenuates myocardial reperfusion injury during brief low flow postischemic infusion. Oxid Med Cell Longev. 2013;2013:279847. doi: 10.1155/2013/279847. Epub 2013 May 22. PubMed PMID: 23766850; PubMed Central PMCID: PMC3674745.