39492-01-8 Usage
Description
GABEXATE, also known as Gabexate Mesylate, is a synthetic protease inhibitor derived from glycerol. It is characterized by its ability to inhibit various proteolytic enzymes, which makes it a promising candidate for pharmaceutical applications. GABEXATE is known for its effectiveness in reducing inflammation and preventing the degradation of proteins.
Source:
GABEXATE is synthesized from glycerol, a widely available and renewable resource.
Production Methods:
GABEXATE is produced through a series of chemical reactions involving glycerol and other reagents, ultimately resulting in the formation of the protease inhibitor.
Uses
Used in Pharmaceutical Industry:
GABEXATE is used as an anti-inflammatory agent for the treatment of acute pancreatitis. It works by inhibiting proteolytic enzymes, which helps to reduce inflammation and prevent further damage to pancreatic tissues.
Used in Elderly Care:
GABEXATE is used in combination with somatostatin and octreotide for the treatment of severe acute pancreatitis in elderly patients. This combination therapy helps to manage the condition more effectively and reduce the risk of complications associated with the disease.
Originator
Gabexate Mesylate,Shangai Lansheng
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
Biological Activity
Serine protease inhibitor; inhibits trypsin, plasmin, plasma kallikrein and thrombin (IC 50 values are 9.4, 30, 41 and 110 mM respectively). Antithrombotic in vitro and in vivo . Also inhibits LPS-induced TNF- α production, probably by inhibiting NF- κ B and AP-1 activation.
Check Digit Verification of cas no
The CAS Registry Mumber 39492-01-8 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,9,4,9 and 2 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 39492-01:
(7*3)+(6*9)+(5*4)+(4*9)+(3*2)+(2*0)+(1*1)=138
138 % 10 = 8
So 39492-01-8 is a valid CAS Registry Number.
InChI:InChI=1/C16H23N3O4.CH4O3S/c1-2-22-15(21)12-7-9-13(10-8-12)23-14(20)6-4-3-5-11-19-16(17)18;1-5(2,3)4/h7-10H,2-6,11H2,1H3,(H4,17,18,19);1H3,(H,2,3,4)
39492-01-8Relevant articles and documents
2-Chloro-1,3-dimethylimidazolinium chloride. 1. A powerful dehydrating equivalent to DCC
Isobe, Toshio,Ishikawa, Tsutomu
, p. 6984 - 6988 (1999)
2-Chloro-1,3-dimethylimidazolinium chloride (DMC) (3) can act as a powerful dehydrating agent, replacing DCC (1) under nearly neutral conditions. Its application to acylation and dehydration is described.