Glybuzole

Names

[ Name ]:
Glybuzole

[Synonym ]:
Gludiase
Glybuzolum [INN-Latin]
glybuzole
EINECS 216-081-2
Desaglybuzol
Glybuzole [INN:JAN]
AN 1324
sulfamidothiodiazol
N-(5-tert-butyl-1,3,4-thiadiazol-2-yl) benzenesulfonamide
RP 7891
Glibuzol [INN-Spanish]
Desaglybuzole
2-Benzolsulfonamino-5-tert.-butyl-1,3,4-thiadiazol

Biological Activity

[Description]:

Glybuzole (Desaglybuzole) is an orally active hypoglycaemic agent that has antidiabetic effect[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[In Vivo]

Glybuzole (100 mg/kg, p.o.) is rapidly absorbed and is found in the serum in concentrations of 100-250 mg/L in dogs and rats[1]. Animal Model: Dogs or rats[1] Dosage: 100 mg/kg Administration: Oral administration (p.o.) Result: Was rapidly absorbed and was found in the serum in concentrations of 100-250 mg/L. Within the 1st few hours, the urinary excretion within 48 h was 15-30% of the administered dose.

[References]

[1]. Populaire P, Terlain B, Lebreton G, et al. Absorption, excretion and biotransformation of benzene sulfonamido-2-tertiobutyl-5-thiadiazole-1, 3, 4 (desaglybuzole= 7 891 RP). Therapie, 1969, 24(2): 313-326.

Chemical & Physical Properties

[ Density]:
1.344g/cm3

[ Boiling Point ]:
449.4ºC at 760mmHg

[ Molecular Formula ]:
C₁₂H₁₅N₃O₂S₂

[ Molecular Weight ]:
297.39600

[ Flash Point ]:
225.6ºC

[ Exact Mass ]:
297.06100

[ PSA ]:
108.57000

[ LogP ]:
3.79020

[ Vapour Pressure ]:
2.88E-08mmHg at 25°C

[ Index of Refraction ]:
1.605

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DB1290000

CHEMICAL NAME :: Benzenesulfonamide, N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)-

CAS REGISTRY NUMBER :: 1492-02-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C12-H15-N3-O2-S2

MOLECULAR WEIGHT :: 297.42

WISWESSER LINE NOTATION :: T5NN DSJ CX1&1&1 EMSWR

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 :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 219 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 310 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 550 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Endocrine - hypoglycemia

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,131,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 235 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 248 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 193 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 967 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 118 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2100 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2100 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1050 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969