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Glisoxepid

Names

[ CAS No. ]:
25046-79-1

[ Name ]:
Glisoxepid

[Synonym ]:
Glisoxepida [INN-Spanish]
Glisepin
Glisoxepida
Glisoxepid
Glisoxepide
5-methyl-isoxazole-3-carboxylic acid 4-(azepan-1-ylcarbamoyl-sulfamoyl)-phenethylamide
Glisoxepida [Spanish]
N-{2-[4-({[(azepan-1-ylamino)carbonyl]amino}sulfonyl)phenyl]ethyl}-5-methylisoxazole-3-carboxamide
Glisoxepidum
Glisoxepidum [INN-Latin]
N-{2-[4-({[(azepan-1-yIamino)carbonyI]amino}suIfonyl)phenyI]ethyI}-5-methylisoxazole-3-carboxamide
Glisoxepide (INN)
Pro-Diaban

Biological Activity

[Description]:

Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Research Areas >> Metabolic Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

K(ATP) channel[1]


[In Vitro]

Glisoxepide inhibits the uptake of bile acids into isolated rat hepatocytes[3]. Glisoxepide noncompetitively inhibits the cholate uptake with a Ki of 200 μM[3].

[References]

[1]. Sato T, et al. Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection. J Pharmacol Exp Ther. 2006 Jan;316(1):182-8. Epub 2005 Sep 20.

[2]. Selvaag E. Photohemolytic potency of oral antidiabetic drugs in vitro: effects of antioxidants and a nitrogen atmosphere. Photodermatol Photoimmunol Photomed. 1996 Aug;12(4):166-70.

[3]. Fückel D, et al. Interaction of sulfonylureas with the transport of bile acids into hepatocytes. Eur J Pharmacol. 1992 Mar 31;213(3):393-404.

Chemical & Physical Properties

[ Density]:
1.37g/cm3

[ Molecular Formula ]:
C20H27N5O5S

[ Molecular Weight ]:
449.52400

[ Exact Mass ]:
449.17300

[ PSA ]:
142.02000

[ LogP ]:
3.92580

[ Index of Refraction ]:
1.617

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NY2350000
CHEMICAL NAME :
3-Isoxazolecarboxamide, N-(2-(4-(((((hexahydro-1H-azepin-1-yl)amino)carbonyl) amino)sulfonyl) phenyl)ethyl)-5-methyl-
CAS REGISTRY NUMBER :
25046-79-1
LAST UPDATED :
199612
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C20-H27-N5-O5-S
MOLECULAR WEIGHT :
449.58
WISWESSER LINE NOTATION :
T7NTJ AMVMSWR D2MV- ET5NOJ C1

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 :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
196 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
283 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds

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