| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Gabexate Mesylate (Megacert; Arodate) is a novel, potent and synthetic inhibitor of serine protease that has anticoagulant properties. With an IC50 of 0.19 μM, it suppresses serine protease and is used to treat disseminated intravascular coagulation and pancreatitis. Human and bovine tryptases' primary specificity site S1 is bound by gabexate mesylate. Gabexate mesylate's carbonyl group interacts with the enzyme's oxyanion binding hole. Gabexate mesylate binds to human tryptase more tightly than it does to bovine tryptase, which leads to a higher affinity.
| Targets |
serine protease (IC50 = 0.19 μM)
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| ln Vitro |
Gabexate mesylate is also discovered to have 150μM and 5mM Ki values for inhibiting cNOS and iNOS. It increases the expression of the iNOS gene. Furthermore, gabexate mesylate has an EC50 value of 250μM, which inhibits the NO production induced by LPS/IFNγ.
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| ln Vivo |
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| Enzyme Assay |
Gabexate mesylate has a Kivalue of 1.0×104M and 5.0×103M, respectively, for competitively constitutive and inducible NO synthase (cNOS and iNOS), at pH 7.4 and 37.0°C. When E. colilipopolysaccharide and interferon-γ are added to rat C6 glioma cells, gabexate mesylate increases the expression of iNOS mRNA. When E. colilipopolysaccharide and interferon-γ are added to rat C6 glioma cells, gabexate mesylate inhibits the production of nitrite (NO release) in a dose-dependent manner.
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| Animal Protocol |
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| References |
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| Additional Infomation |
Gabexate methanesulfonate is a methanesulfonate salt, a member of guanidines and a benzoate ester.
A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin. See also: Gabexate (annotation moved to). |
| Molecular Formula |
C17H27N3O7S
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| Molecular Weight |
417.48
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| Exact Mass |
417.156
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| Elemental Analysis |
C, 48.91; H, 6.52; N, 10.07; O, 26.83; S, 7.68
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| CAS # |
56974-61-9
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| Related CAS # |
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| PubChem CID |
6604561
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| Appearance |
White to off-white solid powder
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| Boiling Point |
508.6ºC at 760 mmHg
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| Melting Point |
91 °C
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| Flash Point |
261.4ºC
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| LogP |
3.587
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
493
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
DNTNDFLIKUKKOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/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)
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| Chemical Name |
ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 130 mg/mL (311.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3953 mL | 11.9766 mL | 23.9532 mL | |
| 5 mM | 0.4791 mL | 2.3953 mL | 4.7906 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3953 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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