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Gabexate mesylate

Product Name
Gabexate mesylate
CAS No.
56974-61-9
Chemical Name
Gabexate mesylate
Synonyms
FOY;Agalit;FOY-007;Arodate;Megacert;MEGACART;GABEXATE;FOY-S 983;Mesyl Gabexate;gabexatomesilato
CBNumber
CB4258638
Molecular Formula
C17H27N3O7S
Formula Weight
417.48
MOL File
56974-61-9.mol
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Gabexate mesylate Property

Melting point:
89.0 to 93.0 °C
form 
solid
Merck 
14,4320
InChIKey
DNTNDFLIKUKKOC-UHFFFAOYSA-N
CAS DataBase Reference
56974-61-9(CAS DataBase Reference)
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Safety

Hazard Codes 
Xn
RIDADR 
3077
WGK Germany 
2
RTECS 
DG2800800
HS Code 
29252900
Toxicity
LD50 in mice (mg/kg): 8000 orally; 4700 s.c.; 25 i.v. (Fujita)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
G2417
Product name
Gabexate mesylate
Purity
analytical standard, for drug analysis
Packaging
5mg
Price
$175
Updated
2020/08/18
TCI Chemical
Product number
G0464
Product name
Gabexate Mesylate
Purity
>97.0%(N)
Packaging
1g
Price
$146
Updated
2020/06/24
TCI Chemical
Product number
G0464
Product name
Gabexate Mesylate
Purity
>97.0%(N)
Packaging
5g
Price
$510
Updated
2020/06/24
Cayman Chemical
Product number
23767
Product name
Gabexate (mesylate)
Purity
≥98%
Packaging
5mg
Price
$65
Updated
2020/06/24
Cayman Chemical
Product number
23767
Product name
Gabexate (mesylate)
Purity
≥98%
Packaging
10mg
Price
$78
Updated
2020/06/24
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Gabexate mesylate Chemical Properties,Usage,Production

Chemical Properties

Gabexate mesylate is supplied as a crystalline solid. A stock solution may be made by dissolving the gabexate (mesylate) in the solvent of choice. Gabexate (mesylate) is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of gabexate (mesylate) in these solvents is approximately 25 mg/ml.
Gabexate is a competitive inhibitor of serine proteases that inhibits human thrombin, urokinase, plasmin, and Factor Xa (Kis = 0.97, 1.3, 1.6, and 8.5 μM, respectively). It also inhibits bovine thrombin, Factor Xa, and trypsin, and porcine plasma kallikrein (Kis = 1.4, 2.1, 2.6, and 0.2 μM, respectively). In vitro, gabexate inhibits clotting activity of thrombin (IC50 = 10 μM).In vivo, it inhibits fibrin formation in rats when administered at a continuous infusion of 120 μmol/kg per hour. Gabexate inhibits LPS-stimulated TNF-α production from monocytes by inhibiting binding of NF-κB and activator protein 1 (AP-1) to target sites and inducing degradation of IκBα.

Originator

Gabexate Mesylate,Shangai Lansheng

Uses

Gabexate Mesylate is a serine protease inhibitor. Gabexate Mesylate inhibits trypsin, plasmin, plasma kallikrein and thrombin. Gabexate Mesylate inhibits lipopolysaccharide-induced tumor necrosis factor-α (TNF-α) production through nuclear factor-κB and activator protein-1 activation.

Uses

Pancreatitis;Serine protease inhibitor.
Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.

Preparation

Guanidinocaproic acid p-tosyl salt and thionyl chloride were mixed together toreact at the room temperature. An endothermic reaction occurred and thecaproic acid gradually dissolved. Then the reaction mixture was left standingfor 1 to 2 h and was extracted with ether. The lower oily layer and the etherlayer were separated from each other and the lower layer was repeatedlywashed with ether. Then the oily substance (caproic acid chloride) was addedwith benzoic acid ethyl ester in tetrahydrofuran, and the mixture was stirred.After the mixture became a uniform solution, of pyridine were graduallyadded. An exothermic reaction occurred and an oily substance came to beseparated in the lower layer. After the completion of the reaction, the oilysubstance was washed with water and then recrystallized from hot water onceor twice. Thus 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl ester salt wasobtained as white crystals.
To obtained the base 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl esterthe 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl ester salt must be treatedby, for example, sodium hydroxide.
In practice it is usually used as gabexate Mesylate.

Manufacturing Process

Guanidinocaproic acid p-tosyl salt and thionyl chloride were mixed together to react at the room temperature. An endothermic reaction occurred and the caproic acid gradually dissolved. Then the reaction mixture was left standing for 1 to 2 h and was extracted with ether. The lower oily layer and the ether layer were separated from each other and the lower layer was repeatedly washed with ether. Then the oily substance (caproic acid chloride) was added with benzoic acid ethyl ester in tetrahydrofuran, and the mixture was stirred. After the mixture became a uniform solution, of pyridine were gradually added. An exothermic reaction occurred and an oily substance came to be separated in the lower layer. After the completion of the reaction, the oily substance was washed with water and then recrystallized from hot water once or twice. Thus 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl ester salt was obtained as white crystals.
To obtained the base 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl ester the 4-(6-guanidino-hexanoyloxy)-benzoic acid ethyl ester salt must be treated by, for example, sodium hydroxide.
In practice it is usually used as mesylate.

Therapeutic Function

Enzyme inhibitor

Mechanism of action

Gabexate mesilate (FOY-007) is a protease inhibitor with a broad spectrum inhibiting not only trypsin and kallikrein, but also plasmin, thrombin,factor Xa, elastase, complement 1 (C1), esterase and phospholipase A2. Prophylactic application of FOY-007 or Camostat mesilate (FOY-305) showed some beneficial effect in CDEinduced pancreatitis, cerulein-induced panceratitis and sodium taurocholate-induced panceratitis. The therapeutic effect of FOY-007 in acute panceratitis has been ascribed to its inhibition of pancreatic enzyme activity, like trypsin, thus preventing autodigestion.

Clinical Use

Gabexate mesylate inhibits proteases and suppresses endothelial cell injury and may be used to treat DIC ascribed to various kinds of diseases.
Therapeutic Function: Enzyme inhibitor

Gabexate mesylate Preparation Products And Raw materials

Raw materials

Preparation Products

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Gabexate mesylate Suppliers

Shanghai Hongbang Pharmaceutical Co., Ltd.
Tel
021-24280809-
Fax
021-24280809
Email
1377976036@qq.com;
Country
China
ProdList
323
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833- ;010-82848833-
Fax
86-10-82849933
Email
jkinfo@jkchemical.com;market6@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15880
Advantage
69
TCI (Shanghai) Development Co., Ltd.
Tel
021-67121386 / 800-988-0390
Fax
021-67121385
Email
Sales-CN@TCIchemicals.com
Country
China
ProdList
24555
Advantage
81
Capot Chemical Co., Ltd
Tel
+86 (0) 571 85 58 67 18
Fax
0086-571-85864795
Email
sales@capotchem.com
Country
China
ProdList
18228
Advantage
66
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
9918
Advantage
62
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
1938
Advantage
70
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070-
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19994
Advantage
64
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15425
Advantage
60
XiaoGan ShenYuan ChemPharm co,ltd
Tel
0712-2580635- ;0712-2580635
Fax
QQ: 1791901229
Email
1791901229@qq.com;1791901229@qq.com;
Country
China
ProdList
8999
Advantage
52
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View Lastest Price from Gabexate mesylate manufacturers

Beijing Yibai Biotechnology Co., Ltd
Product
Gabexate mesylate 56974-61-9
Price
US $0.00-0.00/KG
Min. Order
1g
Purity
99.0%
Supply Ability
500kg/month
Release date
2019-08-28
Shaanxi Dideu Medichem Co. Ltd
Product
Gabexate mesylate 56974-61-9
Price
US $1.00-1.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50tons
Release date
2020-05-06
Shaanxi Dideu Medichem Co. Ltd
Product
Gabexate Mesylate 56974-61-9
Price
US $1.00-0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100000KG
Release date
2020-01-10

56974-61-9, Gabexate mesylateRelated Search:


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