Gabexato mesilato [Spanish]
gabexate mesylate
CAS: 56974-61-9
Molecular Formula: C17H27N3O7S
Gabexato mesilato [Spanish] - Names and Identifiers
Gabexato mesilato [Spanish] - Physico-chemical Properties
| Molecular Formula | C17H27N3O7S |
| Molar Mass | 417.48 |
| Melting Point | 89.0 to 93.0 °C |
| Boling Point | 90-93℃ |
| Solubility | DMSO 83 mg/mL Water 12 mg/mL Ethanol 83 mg/mL |
| Appearance | solid |
| Color | Off-white |
| Merck | 14,4320 |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| 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. |
| MDL | MFCD00210299 |
| Physical and Chemical Properties | White crystals. Soluble in ethanol, chloroform or water, acetone-soluble, a few do not dissolve in ether. Melting point 90-92 °c. Acute toxicity LD50 mice (mg/kg):8000 oral; 4700 subcutaneous injection; 25 intravenous injection. |
Gabexato mesilato [Spanish] - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| UN IDs | 3077 |
| WGK Germany | 2 |
| RTECS | DG2800800 |
| HS Code | 29252900 |
| Toxicity | LD50 in mice (mg/kg): 8000 orally; 4700 s.c.; 25 i.v. (Fujita) |
Gabexato mesilato [Spanish] - Nature
Open Data Verified Data
white crystals. Soluble in ethanol, chloroform or water, acetone-soluble, almost insoluble in ether. Melting point 90-92 °c.
Last Update：2024-01-02 23:10:35
Gabexato mesilato [Spanish] - Preparation Method
Open Data Verified Data
6 amino hexanoic acid and sodium hydroxide reaction, the formation of 6 amino hexanoic acid sodium. And methylisothiourea sulfate aqueous solution reaction, 6 guanidino hexanoic acid. Then, the mixture is stirred with methanesulfonic acid in water, filtered to remove insolubles, concentrated under reduced pressure, added with acetone, placed, and filtered to obtain 6-guanidinohexanoic acid methanesulfonate, which is recrystallized with methanol-diethyl ether. 6 a guanidino hexanoic acid methanesulfonate by thionyl chloride chloride for acid chloride, and then with ethyl p-hydroxybenzoate in tetrahydrofuran and pyridine reaction, after treatment of Gabexate mesylate.
Last Update：2022-01-01 09:23:36
Gabexato mesilato [Spanish] - Standard
Authoritative Data Verified Data
This product is a methanesulfonate of ethyl 4-(6-guanidinohexyloxy) benzoate. The content of C16H23N304 • CH403S shall be between 98.0% and 102.0% calculated as dry.
Last Update：2024-01-02 23:10:35
Gabexato mesilato [Spanish] - Trait
Authoritative Data Verified Data
- This product is white crystal or crystalline powder; Odorless.
- This product is soluble in water or ethanol, and almost insoluble in ethyl acetate or ether.
melting point
The melting point of this product (General rule 0612 first method) is 90~93°C.
Last Update：2022-01-01 11:38:47
Gabexato mesilato [Spanish] - Introduction
gabexate mesylate
Last Update：2022-10-16 17:26:28
Gabexato mesilato [Spanish] - Use
Open Data Verified Data
Japanese Minno pharmaceutical development, approved for marketing in June 2017. Is a non-peptide protein inhibitors, can inhibit trypsin, kallikrein, plasmin, thrombin and other protease activity, so as to prevent the pathophysiological changes caused by these enzymes. It is used for the treatment of acute pancreatitis, acute attack of chronic recurrent pancreatitis, acute pancreatitis complicated after operation, frequent vascular thrombosis and so on.
Last Update：2022-01-01 09:23:36
Gabexato mesilato [Spanish] - Differential diagnosis
Authoritative Data Verified Data
- Take 20mg of this product, according to the oxygen flask combustion method (General rule 0703) for organic destruction, with 1% hydrogen peroxide solution 10ml as absorption liquid, to be fully absorbed, add 2 drops of barium chloride test solution, that is, a white precipitate is produced, separated, and the precipitate is insoluble in hydrochloric acid.
- take this product, add water to make a solution containing about 12ug per lml, according to UV-visible spectrophotometry (General 0401), there is maximum absorption at the wavelength of 236nm, there is minimal absorption at a wavelength of 212nm.
- The infrared absorption spectrum of this product should be consistent with that of the reference product (General rule 0402).
Last Update：2022-01-01 11:38:47
Gabexato mesilato [Spanish] - Safety
Open Data Verified Data
Gabexate mesylate: Mouse LDso(mglkg): 8000 by mouth; 4700 by subcutaneous injection; 25 by intravenous injection.
Last Update：2022-01-01 09:23:37
Gabexato mesilato [Spanish] - Exam
Authoritative Data Verified Data
acidity
take L. 0g of this product, Add 10ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 4.0~6.0.
clarity of the solution
take l.Og of this product, add water to dissolve 5ml, the solution should be clear; If it is turbid, compared with No. 2 Turbidity standard solution (General rule 0902 first method), it should not be more concentrated.
ethyl p-hydroxybenzoate
take an appropriate amount of this product, precision weighing, add methanesulfonic acid methanol solution (take 2ml of 0.48% methanesulfonic acid solution, dilute with methanol to 1000ml) to dissolve and make a solution containing 1 mg per 1 ml, as a test solution; Take the appropriate amount of ethyl p-hydroxybenzoate reference substance, precision weighing, with methanesulfonic acid methanol solution made containing 5ug per 1 mL solution, as a reference solution, in addition to the detection wavelength of 258nm, according to the chromatographic conditions under the content determination item, respectively inject human liquid chromatograph to record the chromatogram by precisely measuring each L01 of the above two solutions. If there is a peak of ethyl p-hydroxybenzoate in the chromatogram of the test solution, the peak area shall be calculated according to the external standard method, and the peak area shall not exceed 0.5%.
residual solvent
take about lg of this product, put it in a 10ml measuring flask, add water to dissolve and dilute to the scale, shake well, and use it as a stock solution for test. Take 1ml for precision measurement and place it in the top empty bottle, precision Add 1ml water, shake, seal, as a test solution; Another precision weigh acetone 0.25g, put 50ml measuring flask, add water to dissolve and dilute to the scale, shake, take 10ml accurately, put it in a 100ml measuring flask, dilute it to the scale with water, shake it well, and use it as the reference stock solution; Take 1ml of the reference stock solution accurately, put it in the top empty bottle, and add lml of water precisely, shake, seal, as a control solution. According to the determination method of residual solvent (General rule 0861, the first method), the capillary column with 100% dimethylpolysiloxane (or similar polarity) as the stationary liquid is used as the column, the column temperature is 40°C, and the column temperature is maintained for 12 minutes, the temperature of the detector is 250°C; The temperature of the injection port is 200°C; The equilibrium temperature of the headspace bottle is 70°C, and the equilibrium time is 30 minutes; The control solution is injected into the headspace, calculate the results of several injection, the relative standard deviation should not exceed 5.0%, take the sample solution and the reference solution respectively, record the chromatogram, and calculate the peak area according to the external standard method, the residual amount of acetone should be in accordance with the regulations.
chloride
take this product l. Add 50ml of water to dissolve, add 2ml of nitric acid, shake well, place for 5 minutes, filter, take 25ml of filtrate, check according to law (General rule 0801), and standard sodium chloride solution 5.0ml of the control solution should not be more concentrated (0.01%).
sulfate
take 0.50g of this product and check it according to law (General rule 0802). Compared with the control solution made of 0.05% of standard potassium sulfate solution, it should not be more concentrated ().
loss on drying
taking this product, using phosphorus pentoxide as desiccant, drying under reduced pressure at 60°C for 4 hours, the weight loss shall not exceed 0.3% (General rule 0831).
burning residue
not more than 0.1% (General rule 0841).
Heavy metals
take 0.50g of this product, Add 10ml of water to dissolve, add 5ml of sodium hydroxide solution, add water to 25ml, shake, filter, take the filtrate, check according to law (General rule 0821 method), heavy metals should not be more than 20 parts per million.
Last Update：2022-01-01 11:38:48
Gabexato mesilato [Spanish] - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel was bonded with octanoalkyl silane as filler; 4ml of methanol-sodium acetate buffer solution [acetic acid-sodium acetate buffer (pH 3.6), dilute to 100ml with water]-sodium dodecyl sulfate solution (take 5g of sodium dodecyl sulfate, dissolve and dilute to 100ml with 50% methanol solution)-sodium heptane sulfonate solution (take 5g of sodium heptane sulfonate, add 50% methanol solution to dissolve and dilute to 300 ml)-Isopropanol (150: 1, 2:2:2:8) as mobile phase; The detection wavelength was 236nm, the number of theoretical plates is not less than 2000 calculated from the Gabexate peak.
assay
ready to use new system, and below 25°C storage. Take about 15mg of this product, accurately weigh it, put it in a 50ml measuring flask, add methanesulfonic acid methanol solution (take 2ml of 0.48% methanesulfonic acid solution, dilute it to ML with methanol), dissolve it and dilute it to the scale, shake it well, 10u1 was injected into human liquid chromatograph, and the chromatogram was recorded. About 15mg of the reference substance of Gabexate mesylate was obtained, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:38:49
Gabexato mesilato [Spanish] - Category
Authoritative Data Verified Data
protease inhibitors.
Last Update：2022-01-01 11:38:49
Gabexato mesilato [Spanish] - Storage
Authoritative Data Verified Data
sealed, stored in the cool dark.
Last Update：2022-01-01 11:38:49
Gabexato mesilato [Spanish] - Gabexate Mesilate for Injection
Authoritative Data Verified Data
This product is a sterile freeze-dried product made of an appropriate amount of Gabexate Mesylate and mannitol. The content of Gabexate mesylate C16H23N304 • CH4C)3S shall be between 90.0% and 110.0% of the labeled amount calculated as the average loading.
trait
This product is white or off-white lyophilized cake or powder.
identification
- take this product and make a solution containing about 10ug per lml of water. According to UV-Vis spectrophotometry (General 0401), there is maximum absorption at the wavelength of 236nm, there is minimal absorption at a wavelength of 212nm.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
examination
- acidity take 1 bottle of this product, add 10ml of water for injection, dissolve, shake well, and check according to law (General rule 0631), the pH value should be 4.0~5.0. Ethyl p-hydroxybenzoate take appropriate amount of this product, precision weighing, add methanesulfonic acid methanol solution (take 2ml of 0.48% methanesulfonic acid solution, dilute with methanol to 1000ml) dissolve and make a solution containing 1 mg per 1 ml, as a test solution; In addition, an appropriate amount of ethyl p-hydroxybenzoate reference substance was accurately weighed, and a solution containing 5ug per 1 ml of methanesulfonic acid methanol solution was prepared as a reference solution. According to the chromatographic conditions under the content determination item, the detection wavelength is 258Nm. Take each L01 of the above two solutions and inject them into the liquid chromatograph respectively, and record the chromatogram. If there is a peak of ethyl p-hydroxybenzoate in the chromatogram of the test solution, the peak area shall be calculated according to the external standard method, and 0.5% of the labeled amount of Gabexate mesylate shall not be exceeded.
- Related substances are newly prepared and stored below 25°C. Take appropriate amount of this product, precision weighing, add methanesulfonic acid methanol solution (take 0.48% methanesulfonic acid solution 2ml, dilute with methanol to 1000ml) dissolve and prepare the solution containing 1 mg per 1ml as the test solution; Take 1ml of the test solution with precision, put it in a 100ml measuring flask, add methanesulfonic acid methanol solution to dissolve and dilute to the scale, as a control solution. According to the chromatographic condition test under the content determination item, take 10ul of the test solution and the control solution, respectively inject the human liquid chromatograph, record the chromatogram to 3 times the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area (except the ethyl p-hydroxybenzoate peak) shall not be greater than the main peak area of the control solution (1.0%).
- weight loss on drying this product shall be dried under reduced pressure at 60°C for 6 hours with phosphorus pentoxide as desiccant, and the weight loss shall not exceed 1.0% (General rule 0831).
- the pyrogen is to take the product and add Sterile Water for Injection to make a solution containing 10 mg of Gabexate mesylate per 1ml, which shall be checked according to law (General rule 1142), and the dose shall be 1ml per 1kg of rabbit body weight for slow injection, the requirements shall be met.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; With methanol-sodium acetate buffer solution [acetic acid-sodium acetate buffer (pH 3.6 )4ml, dilute with water to 100ml]-sodium dodecyl sulfate solution (take 5g of sodium dodecyl sulfate, add 50% methanol solution to dissolve and dilute to lOOmD-sodium heptane sulfonate solution (take 5g of sodium heptane sulfonate, add 50% methanol solution to dissolve and dilute to 300 ml) -Isopropanol (150: 1, 2:2:2:8) as mobile phase; The detection wavelength was 236nm, the number of theoretical plates is not less than 2000 calculated from the Gabexate peak.
- The assay is freshly prepared, and the contents under the item of <25°C are stored & removed, mixed evenly, and the appropriate amount (equivalent to about 15mg of Gabexate mesylate) is accurately weighed, add methanesulfonic acid methanol solution (take 2ml of 0.48% methanesulfonic acid solution, dilute to ML with methanol) into a 50ml measuring flask, dilute to the scale, shake well, and use as a test solution, 10ul was injected into the liquid chromatograph, and the chromatogram was recorded. About 15mg of the reference substance of Gabexate mesylate was obtained, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
with Gabexate mesylate.
specification
O.lg
storage
sealed and kept in a cool dark place.
Last Update：2022-01-01 11:38:50
Gabexato mesilato [Spanish] - Reference Information
| biological activity | Gabexate Mesylate is a serine protease inhibitor with an IC50 of 0.19 μm for the treatment of pancreatitis and Disseminate Intravascular Coagulation. |
| Target | Value |
| serine protease | 0.19 μM |
| Use | non-peptide proteolytic enzyme inhibitors. It is used for the treatment of acute pancreatitis, acute attack of chronic recurrent pancreatitis, acute pancreatitis complicated after operation, frequent vascular thrombosis and so on. Gabexate is a kind of non-peptide protein inhibitor, which can inhibit the activity of trypsin, kallikrein, plasmin, thrombin and other proteases, so as to stop the pathophysiological changes caused by these enzymes. In experimental acute pancreatitis, activated trypsin was inhibited, pancreatic injury was alleviated, and serum amylase, lipase activity and urea nitrogen increased significantly. Gabexate Mesylate is a serine protease inhibitor. Gabexate Mesylate inhibits trypsin, plasmin, plasma kallikrein and thrombin. Gabexate Mesylate inhibits lipopolysaccharide-induced tumor necrosis fact or-α (TNF-α) production through nuclear factor-κB and activator protein-1 activation. |
| production method | the reaction of 6-aminocaproic acid and sodium hydroxide produces sodium 6-aminocaproate. Further, it is reacted with an aqueous solution of methylisothiourea sulfate to obtain 6-guanidinohexanoic acid. Then, the mixture was stirred with methanesulfonic acid in water, filtered to remove insolubles, concentrated under reduced pressure, added with acetone, placed and filtered to obtain 6-guanidinohexanoic acid methanesulfonate, which was recrystallized with methanol-diethyl ether, the melting point was 116-118 °c. 6-guanidinohexanoic acid methanesulfonate was chlorinated to acid chloride via sulfoxide chloride, and then reacted with ethyl p-hydroxybenzoate in tetrahydrofuran and pyridine to obtain Gabexate mesylate. |
Last Update：2024-04-09 20:49:11
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CAS: 56974-61-9
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Mobile: 18021002903
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