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
- Molecular Weight:
- 417.48
- MOL File:
- 56974-61-9.mol
- Modify Date:
- 2023/6/30 15:45:59
| 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
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Warning |
| Hazard statements | H373 |
| Precautionary statements | P260-P314-P501 |
| 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) |
Gabexate mesylate price More Price(2)
Gabexate mesylate Chemical Properties,Uses,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.
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.
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
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| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| TCI Chemicals (India) Pvt. Ltd. | 1800 425 7889 | New Delhi, India | 6778 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | China | 9338 | 55 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29900 | 58 | Inquiry |
| Xiamen AmoyChem Co., Ltd | +86-592-6051114 +8618959220845 | China | 6387 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49391 | 58 | Inquiry |
| SIMAGCHEM CORP | +86-13806087780 | China | 17367 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
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