Title: Sepimostat
CAS Registry Number: 103926-64-3
CAS Name: 4-[(4,5-Dihydro-1H-imidazol-2-yl)amino]benzoic acid 6-(aminoiminomethyl)-2-naphthalenyl ester
Additional Names: 6-amidino-2-naphthyl p-(2-imidazolin-2-ylamino)benzoate
Molecular Formula: C21H19N5O2
Molecular Weight: 373.41
Percent Composition: C 67.55%, H 5.13%, N 18.76%, O 8.57%
Literature References: Nonpeptide serine protease inhibitor; structural analog of nafamostat. Prepn: S. Fujii et al., WO 8600893; eidem, US 4777182 (1986, 1988 both to Torii); T. Nakayama et al., Chem. Pharm. Bull. 41, 117 (1993). Enzyme inhibitory activity: M. Oda et al., Jpn. J. Pharmacol. 52, 23 (1990). Effects on exptl pancreatitis: H. Murakami et al., Arzneim.-Forsch. 40, 1352 (1990). HPLC determn in biological fluids: T. Marunaka et al., J. Chromatogr. 433, 177 (1988). Toxicity study: K. Terazawa et al., J. Toxicol. Sci. 17, Suppl. 4, 1 (1992).
Derivative Type: Methanesulfonate
CAS Registry Number: 103926-82-5
Additional Names: Sepimostat mesylate
Manufacturers' Codes: FUT-187; TO-187
Trademarks: Renofuthan (Torii)
Molecular Formula: C21H19N5O2.2CH3SO3H
Molecular Weight: 565.62
Percent Composition: C 48.84%, H 4.81%, N 12.38%, O 22.63%, S 11.34%
Properties: Crystals from water-ethanol, mp 248-250°. Sol in water. LD50 in male, female mice, male, female rats (mg/kg): 39.4, 41.4, 21.8, 15.8 i.v.; 6284, 5492, 6799, 3343 s.c.; 4395, 3626, 4653, 3761 orally (Terazawa).
Melting point: mp 248-250°
Toxicity data: LD50 in male, female mice, male, female rats (mg/kg): 39.4, 41.4, 21.8, 15.8 i.v.; 6284, 5492, 6799, 3343 s.c.; 4395, 3626, 4653, 3761 orally (Terazawa)
Therap-Cat: Protease inhibitor.
Keywords: Protease Inhibitor.
Status: This monograph has been retired and is no longer subject to revision or update. |