Sivelestat Sodium | CAS#201677-61-4 | elastase inhibitor

MedKoo Cat#: 563557 | Name: Sivelestat Sodium hydrate

Description:

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

Sivelestat Sodium is an inhibitor of human neutrophil elastase.

Chemical Structure

Sivelestat Sodium hydrate

CAS#201677-61-4 (sodium hydrate)

Theoretical Analysis

MedKoo Cat#: 563557

Name: Sivelestat Sodium hydrate

CAS#: 201677-61-4 (sodium hydrate)

Chemical Formula: C20H29N2NaO11S

Exact Mass: 0.0000

Molecular Weight: 528.50

Elemental Analysis: C, 45.45; H, 5.53; N, 5.30; Na, 4.35; O, 33.30; S, 6.07

Price and Availability

Size	Price	Availability
50mg	USD 90.00	Ready to ship
100mg	USD 150.00	Ready to ship
250mg	USD 250.00	Ready to ship
500mg	USD 350.00	Ready to ship
1g	USD 550.00	Ready to ship
2g	USD 850.00	Ready to ship
5g	USD 1,750.00	Ready to ship
10g	USD 2,750.00	Ready to ship
20g	USD 4,450.00	Ready to ship

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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 Hydrate; Sivelestat sodium tetrahydrate; ONO-5046; ONO 5046; ONO5046; Elaspol;

IUPAC/Chemical Name

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

InChi Key

PLHREJBSQUSUCW-UHFFFAOYSA-M

InChi Code

InChI=1S/C20H22N2O7S.Na.4H2O/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);;4*1H2/q;+1;;;;/p-1

SMILES Code

O=C([O-])CNC(C1=CC=CC=C1NS(=O)(C2=CC=C(OC(C(C)(C)C)=O)C=C2)=O)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+]

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

Shelf Life

>3 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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot# C20R12B29

QC Data

View QC data: current batch, Lot# C20R12B29

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Sivelestat is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM.

In vitro activity:

The combination of sivelestat and trastuzumab might be a novel therapeutic strategy for HER2-positive breast cancer. Sivelestat effectively suppressed the tumor progression mechanism initiated by neutrophil elastase (NE) through tumor growth factor-α (TGF-α) in breast cancer cells, while the impact of trastuzumab was hindered by TGF-α. However, the combination of trastuzumab and sivelestat resulted in more potent suppression of cell proliferation, overcoming the impairment by TGF-α on HER2 down-regulation. Reference: Anticancer Res. 2012 Jan;32(1):13-9. https://pubmed.ncbi.nlm.nih.gov/22213283/

In vivo activity:

Sivelestat attenuated AngII-induced abdominal aortic aneurysm through the inhibition of neutrophil elastase. In the 1-week study in male apolipoprotein E-deficient mice, AngII increased plasma and tissue elastase activity and aortic width, which were reduced by sivelestat. Sivelestat also decreased the incidence of abdominal aortic aneurysms and mitigated elastin fragmentation induced by AngII. Inflammatory cell accumulation and MMP-2/9 enhancement by AngII were reduced by sivelestat. Reference: Am J Hypertens. 2023 Nov 20:hpad107. https://pubmed.ncbi.nlm.nih.gov/37982444/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	72.0	136.23

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 528.50 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

Formulation protocol:

1. Amaral A, Fernandes C, Rebordão MR, Szóstek-Mioduchowska A, Lukasik K, Gawronska-Kozak B, Telo da Gama L, Skarzynski DJ, Ferreira-Dias G. The In Vitro Inhibitory Effect of Sivelestat on Elastase Induced Collagen and Metallopeptidase Expression in Equine Endometrium. Animals (Basel). 2020 May 16;10(5):863. doi: 10.3390/ani10050863. PMID: 32429399; PMCID: PMC7278485. 2. Nawa M, Osada S, Morimitsu K, Nonaka K, Futamura M, Kawaguchi Y, Yoshida K. Growth effect of neutrophil elastase on breast cancer: favorable action of sivelestat and application to anti-HER2 therapy. Anticancer Res. 2012 Jan;32(1):13-9. PMID: 22213283. 3. Hada Y, Uchida HA, Okamoto S, Otaka N, Katayama K, Subramanian V, Daugherty A, Wada J. Neutrophil Elastase Inhibition by Sivelestat (ONO-5046) Attenuates AngII-induced Abdominal Aortic Aneurysms in Apolipoprotein E-Deficient Mice. Am J Hypertens. 2023 Nov 20:hpad107. doi: 10.1093/ajh/hpad107. Epub ahead of print. PMID: 37982444. 4. Weng J, Liu D, Shi B, Chen M, Weng S, Guo R, Zhou X. Sivelestat sodium alleviated lipopolysaccharide-induced acute lung injury by improving endoplasmic reticulum stress. Gene. 2023 Oct 30;884:147702. doi: 10.1016/j.gene.2023.147702. Epub 2023 Aug 9. PMID: 37567453.

In vitro protocol:

In vivo protocol:

1. Hada Y, Uchida HA, Okamoto S, Otaka N, Katayama K, Subramanian V, Daugherty A, Wada J. Neutrophil Elastase Inhibition by Sivelestat (ONO-5046) Attenuates AngII-induced Abdominal Aortic Aneurysms in Apolipoprotein E-Deficient Mice. Am J Hypertens. 2023 Nov 20:hpad107. doi: 10.1093/ajh/hpad107. Epub ahead of print. PMID: 37982444. 2. Weng J, Liu D, Shi B, Chen M, Weng S, Guo R, Zhou X. Sivelestat sodium alleviated lipopolysaccharide-induced acute lung injury by improving endoplasmic reticulum stress. Gene. 2023 Oct 30;884:147702. doi: 10.1016/j.gene.2023.147702. Epub 2023 Aug 9. PMID: 37567453.

1: Okamoto H, Onodera K, Kamba R, Taniyama Y, Sakurai T, Heishi T, Teshima J, Hikage M, Sato C, Maruyama S, Onodera Y, Ishida H, Kamei T. Treatment of spontaneous esophageal rupture (Boerhaave syndrome) using thoracoscopic surgery and sivelestat sodium hydrate. J Thorac Dis. 2018 Apr;10(4):2206-2212. doi: 10.21037/jtd.2018.03.136. PubMed PMID: 29850124; PubMed Central PMCID: PMC5949456. 2: Pu S, Wang D, Liu D, Zhao Y, Qi D, He J, Zhou G. Effect of sivelestat sodium in patients with acute lung injury or acute respiratory distress syndrome: a meta-analysis of randomized controlled trials. BMC Pulm Med. 2017 Nov 21;17(1):148. doi: 10.1186/s12890-017-0498-z. PubMed PMID: 29162066; PubMed Central PMCID: PMC5699178. 3: Ogawa R, Mori R, Iida K, Uchida Y, Oshiro M, Kageyama M, Kato Y, Tanaka T, Nakata Y, Nishimura Y, Hokuto I, Bonno M, Matsumoto N, Ito M, Takahashi N, Namba F. Effects of the early administration of sivelestat sodium on bronchopulmonary dysplasia in infants: A retrospective cohort study. Early Hum Dev. 2017 Dec;115:71-76. doi: 10.1016/j.earlhumdev.2017.09.016. Epub 2017 Sep 23. PubMed PMID: 28950234. 4: Yu X, Zhao L, Yu Z, Yu C, Bi J, Sun B, Cong H. Sivelestat sodium hydrate improves post-traumatic knee osteoarthritis through nuclear factor-κB in a rat model. Exp Ther Med. 2017 Aug;14(2):1531-1537. doi: 10.3892/etm.2017.4684. Epub 2017 Jun 27. PubMed PMID: 28810618; PubMed Central PMCID: PMC5526152. 5: Kumar H, Jo MJ, Choi H, Muttigi MS, Shon S, Kim BJ, Lee SH, Han IB. Matrix Metalloproteinase-8 Inhibition Prevents Disruption of Blood-Spinal Cord Barrier and Attenuates Inflammation in Rat Model of Spinal Cord Injury. Mol Neurobiol. 2018 Mar;55(3):2577-2590. doi: 10.1007/s12035-017-0509-3. Epub 2017 Apr 18. PubMed PMID: 28421532. 6: Kishimoto M, Yamana H, Inoue S, Noda T, Myojin T, Matsui H, Yasunaga H, Kawaguchi M, Imamura T. Sivelestat sodium and mortality in pneumonia patients requiring mechanical ventilation: propensity score analysis of a Japanese nationwide database. J Anesth. 2017 Jun;31(3):405-412. doi: 10.1007/s00540-017-2327-1. Epub 2017 Feb 27. PubMed PMID: 28243749. 7: Tanaka KI, Tamura F, Sugizaki T, Kawahara M, Kuba K, Imai Y, Mizushima T. Evaluation of Lecithinized Superoxide Dismutase for the Prevention of Acute Respiratory Distress Syndrome in Animal Models. Am J Respir Cell Mol Biol. 2017 Feb;56(2):179-190. doi: 10.1165/rcmb.2016-0158OC. PubMed PMID: 27668315. 8: Huo J, Zhu XL, Ma R, Dong HL, Su BX. GAPDH/Siah1 cascade is involved in traumatic spinal cord injury and could be attenuated by sivelestat sodium. Neuroscience. 2016 Aug 25;330:171-80. doi: 10.1016/j.neuroscience.2016.05.054. Epub 2016 May 30. PubMed PMID: 27256506. 9: Xia H, Sun Z, Yang Y, Shang Y, Yao S. [Effect of sivelestat sodium on the prognosis of patients with acute lung injury and acute respiratory distress syndrome: a meta-analysis]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Oct;27(10):800-4. Chinese. PubMed PMID: 27132441. 10: 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;20(3):528-36. PubMed PMID: 26914130. 11: 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. 12: Sakai H, Sagara A, Matsumoto K, Jo A, Hirosaki A, Takase K, Sugiyama R, Sato K, Ikegami D, Horie S, Matoba M, Narita M. Neutrophil recruitment is critical for 5-fluorouracil-induced diarrhea and the decrease in aquaporins in the colon. Pharmacol Res. 2014 Sep;87:71-9. doi: 10.1016/j.phrs.2014.05.012. Epub 2014 Jun 25. PubMed PMID: 24972040. 13: 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. 14: Shioya Y, Katakura K, Ohira H. Neutrophil elastase inhibitor suppresses IL-17 based inflammation of murine experimental colitis. Fukushima J Med Sci. 2014;60(1):14-21. Epub 2014 Mar 27. PubMed PMID: 24670675. 15: Sakai M, Takenami T, Otsuka T, Hayashi N, Yoshino K, Matsumoto S, Okamoto H. [Anesthetic management of posterior lumbar spinal fusion in a patient suspected of having acute exacerbation of chronic interstitial pneumonia]. Masui. 2014 Feb;63(2):168-71. Japanese. PubMed PMID: 24601111. 16: Ito H, Nakayama H, Yokose T, Yamada K. Prophylaxis for acute exacerbation of interstitial pneumonia after lung resection. Asian Cardiovasc Thorac Ann. 2014 Oct;22(8):948-54. doi: 10.1177/0218492314526187. Epub 2014 Feb 20. PubMed PMID: 24585320. 17: 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. 18: 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. 19: Izumida H, Fujishima S. [Pharmacological therapies for ARDS]. Masui. 2013 May;62(5):541-6. Review. Japanese. PubMed PMID: 23772527. 20: Yoshikawa N, Inomata T, Okada Y, Shimbo T, Takahashi M, Akita K, Uesugi Y, Narumi Y. Sivelestat sodium hydrate reduces radiation-induced lung injury in mice by inhibiting neutrophil elastase. Mol Med Rep. 2013 Apr;7(4):1091-5. doi: 10.3892/mmr.2013.1318. Epub 2013 Feb 8. PubMed PMID: 23404144.