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
Gabexate mesylate Property
- Melting point:
- 89.0 to 93.0 °C
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- Soluble in DMSO (up to 50 mg/ml) or in Water (up to 50 mg/ml).
- form
- solid
- color
- Off-white
- Water Solubility
- Soluble to 100 mM in water
- Merck
- 14,4320
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 1 month.
- InChIKey
- DNTNDFLIKUKKOC-UHFFFAOYSA-N
- CAS DataBase Reference
- 56974-61-9(CAS DataBase Reference)
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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H373May cause damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P314Get medical advice/attention if you feel unwell.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- G2417
- Product name
- Gabexate mesylate
- Purity
- analytical standard, for drug analysis
- Packaging
- 5mg
- Price
- $206
- Updated
- 2022/05/15
- Product number
- G0464
- Product name
- Gabexate Mesylate
- Purity
- >97.0%(N)
- Packaging
- 1g
- Price
- $193
- Updated
- 2024/03/01
- Product number
- G0464
- Product name
- Gabexate Mesylate
- Purity
- >97.0%(N)
- Packaging
- 5g
- Price
- $490
- Updated
- 2021/12/16
- Product number
- 23767
- Product name
- Gabexate (mesylate)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 23767
- Product name
- Gabexate (mesylate)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $96
- Updated
- 2024/03/01
Gabexate mesylate Chemical Properties,Usage,Production
Description
Gabexate mesylate (56974-61-9) is a? serine protease inhibitor inhibiting plasmin, kallikrein, thrombin as well as trypsin, which attenuates pancreatic fibrosis.1? Reduces weight gain and improves metabolism in obese rodent models.2?In clinical use (in Japan) for pancreatitis.3?Inhibits influenza virus replication in human tracheal epithelial cells.4?Reduces infection of Calu-3 lung cells by SARS-CoV-2 (responsible for COVID-19) via inhibition of the serine protease TMPRSS2 required for viral spike protein priming.5
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. Neuroresearch & Neuroprotective Product.
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.
Definition
ChEBI: Gabexate methanesulfonate is a methanesulfonate salt, a member of guanidines and a benzoate ester.
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
storage
Desiccate at RT
References
1) Gibo?et al.?(2005),?Camostat Mesilate Attenuates Pancreatic Fibrosis via Inhibition of Monocytes and Pancreatic Stellate Cells Activity; Lab Invest.,?85?75 2) Albarazanji?et al.?(2019),?Intestinal Serine Protease Inhibition Increases FGF21 and Improves Metabolism in Obese Mice; Am. J. Physiol. Gastrointest. Liver Physiol.,?316?G653 3) Ueda?et al.?(2015),?The Serine Protease Inhibitor Camostat Mesilate Attenuates the Progression of Chronic Kidney Disease Through Its Antioxidant Effects; Nephron,?129?223 4) Yamaya?et al.?(2015),?The Serine Protease Inhibitor Camostat Inhibits Influenza Virus Replication and Cytokine Production in Primary Cultures of Human Tracheal Epithelial Cells; Pulm. Pharmacol. Ther., 33?66 5) Hoffmann?et al.?(2020),?SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor; Cell,?181?271
Gabexate mesylate Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Gabexate mesylate manufacturers
- 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
- Product
- Gabexate mesylate 56974-61-9
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 0.999
- Supply Ability
- 100 Tons min
- Release date
- 2021-08-03
- Product
- Gabexate mesylate 56974-61-9
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10