Gabexate mesylate
Based on 4 publication(s) in Google Scholar
Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation.
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- Pureté: 98.64%
- CAS No.: 56974-61-9
- Formule: C17H27N3O7S
- Masse moléculaire:417.48
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Gabexate mesylate
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Activité biologique
Gabexate mesylate (FOY; 100-1000 μM; 72 hours) decreases The proliferation rate in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:100, 300, and 1000 μM
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Incubation Time:72 hours
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Result:The proliferation rate decreased in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (100-120 g) with spinal nerve ligation (SNL)[4]
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Dosage:20 mg/kg
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Administration:Intraperitoneally; daily; from 3rd day until the 14th day
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Result:Showed a higher PWT than those of the vehicle-treated group.
Markedly decreased the expression of p65.
Attenuated the expressions of IL-1, IL-6, and TNF-α at 7th day.
Chemical Information
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CAS No. 56974-61-9
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Appearance Solid
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Masse moléculaire 417.48
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Formule C17H27N3O7S
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Color White to off-white
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SMILES
O=C(OCC)C1=CC=C(OC(CCCCCNC(N)=N)=O)C=C1.CS(=O)(O)=O
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Synonyms
FOY
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2024 May;11(20):e2308131. PMID: 38498770 -
Eur J Pharmacol
Mechanisms of acid-sensing ion channels inhibition by nafamostat, sepimostat and diminazene. [Abstract]2023 Jan 5:938:175394. PMID: 36403685 -
Eur J Pharmacol
2022 Mar 15:919:174795. PMID: 35122868 -
Tissue Eng Part C Methods
Evaluation of Different Decellularization Protocols on the Generation of Pancreas-Derived Hydrogels. [Abstract]2018 Dec;24(12):697-708. PMID: 30398401
Solvant et solubilité
DMSO : ≥ 100 mg/mL (239.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 7.14 mg/mL (17.10 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 130 mg/mL (311.39 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. H Ohno, et al. FOY: [ethyl P-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. Thromb Res. 1980;19(4-5):579-88. [Content Brief]
[2]. F Erba, et al. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61(3):271-6. [Content Brief]
[3]. Tsuneo Ozeki, et al. The specific inhibition of HepG2 cells proliferation by apoptosis induced by gabexate mesilate. Int J Clin Exp Pathol. 2010 Aug 15;3(7):710-7. [Content Brief]
[4]. Seon Hee Oh, et al. Gabexate mesilate ameliorates the neuropathic pain in a rat model by inhibition of proinflammatory cytokines and nitric oxide pathway via suppression of nuclear factor-κB. Korean J Pain. 2020 Jan 1;33(1):30-39. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3953 mL | 11.9766 mL | 23.9532 mL | 59.8831 mL |
| 5 mM | 0.4791 mL | 2.3953 mL | 4.7906 mL | 11.9766 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3953 mL | 5.9883 mL | |
| 15 mM | 0.1597 mL | 0.7984 mL | 1.5969 mL | 3.9922 mL | |
| DMSO | 20 mM | 0.1198 mL | 0.5988 mL | 1.1977 mL | 2.9942 mL |
| 25 mM | 0.0958 mL | 0.4791 mL | 0.9581 mL | 2.3953 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7984 mL | 1.9961 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4971 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4791 mL | 1.1977 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9981 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7485 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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