Title: Sivelestat
CAS Registry Number: 127373-66-4
CAS Name: N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]glycine
Additional Names: N-[o-(p-pivaloyloxybenzene)sulfonylaminobenzoyl]glycine; N-[2-[4-(2,2-dimethylpropionyloxy)phenylsulfonylamino]benzoyl]aminoacetic acid
Molecular Formula: C20H22N2O7S
Molecular Weight: 434.46
Percent Composition: C 55.29%, H 5.10%, N 6.45%, O 25.78%, S 7.38%
Literature References: Neutrophil elastase inhibitor. Prepn: K. Imaki et al., EP 347168; eidem, US 5017610 (1989, 1991 both to Ono); and structure-activity study: K. Imaki et al., Bioorg. Med. Chem. 4, 2115 (1996). Pharmacology: K. Kawabata et al., Biochem. Biophys. Res. Commun. 177, 814 (1991). HPLC determn in plasma and urine: T. Shintani et al., J. Pharm. Biomed. Anal. 12, 397 (1994). Pharmacokinetics and metabolism in rats: F. Watanabe et al., Biol. Pharm. Bull. 20, 392 (1997). Enzyme inhibition in ex vivo human pleural effusion: T. Sakuma et al., Eur. J. Pharmacol. 353, 273 (1998). Acute toxicity: H. Yanagi et al., J. Toxicol. Sci. 23, Suppl. 3, 409 (1998), C.A. 130, 20355 (1998). Review: L. Pradella, Curr. Opin. Anti-Inflam. Immunomod. Invest. Drugs1, 485-501 (1999).
Properties: mp 218-220°.
Melting point: mp 218-220°
Derivative Type: Sodium salt tetrahydrate
CAS Registry Number: 201677-61-4; 150374-95-1 (anhydrous)
Manufacturers' Codes: EI-546; ONO-5046
Trademarks: Elaspol (Ono)
Molecular Formula: C20H21N2NaO7S.4H2O
Molecular Weight: 528.51
Percent Composition: C 45.45%, H 5.53%, N 5.30%, Na 4.35%, O 33.30%, S 6.07%
Properties: LD50 in rats (mg/kg): 450 i.v. (Yanagi).
Toxicity data: LD50 in rats (mg/kg): 450 i.v. (Yanagi)
Therap-Cat: In treatment of lung injury resulting from systemic inflammatory response syndrome.

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