*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : DG8576110
CHEMICAL NAME : Benzoic acid,
4-((4,5-dihydro-1H-imidazol-2-yl)amino)-,
6-(aminoiminomethyl)-2- naphthalenyl ester,
dimethanesulfonate
CAS REGISTRY NUMBER : 103926-82-5
LAST UPDATED : 199709
DATA ITEMS CITED : 16
MOLECULAR FORMULA : C21-H19-N5-O2.2C-H4-O3-S
MOLECULAR WEIGHT : 565.67
COMPOUND DESCRIPTOR : Drug
Mutagen
Reproductive Effector
SYNONYMS/TRADE NAMES :
* 6-Amidino-2-naphthyl 4-((4,5-dihydro-1H-imidazol-2-yl)amino)benzoate
dimethanesulfonate
* FUT 187
* Sepimostat mesilate
* TO-187
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 3761 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 3343 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 15800 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 3626 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 5492 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 19 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4820730
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 3 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),1,1992
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 114 gm/kg/13W-I
TOXIC EFFECTS :
Gastrointestinal - changes in pancreatic weight
Blood - changes in leukocyte (WBC) count
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - transaminases
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),17,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 18200 mg/kg/52W-I
TOXIC EFFECTS :
Gastrointestinal - changes in pancreatic weight
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),125,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 4550 mg/kg/13W-I
TOXIC EFFECTS :
Gastrointestinal - other changes
Kidney, Ureter, Bladder - other changes
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - transaminases
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),61,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 10920 mg/kg/52W-I
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),163,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 12285 mg/kg/13W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes primarily in glomeruli
Nutritional and Gross Metabolic - weight loss or decreased weight gain
Related to Chronic Data - death
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),101,1992
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 60480 mg/kg
SEX/DURATION : male 9 week(s) pre-mating
female 2 week(s) pre-mating - 7 day(s) after
conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - other measures of fertility
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),201,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 19440 mg/kg
SEX/DURATION : female 17-21 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth)
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
Reproductive - Effects on Newborn - delayed effects
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),263,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 1300 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 17(Suppl
4),253,1992
** MUTATION DATA **
TYPE OF TEST : Mutation in microorganisms
TEST SYSTEM : Bacteria - Salmonella typhimurium
DOSE/DURATION : 19500 ng/plate
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 28,675,1994
*** END OF RECORD ***