kininogenin
kallikrein from human plasma
CAS: 9001-01-8
Molecular Formula:
kininogenin - Names and Identifiers
kininogenin - Physico-chemical Properties
| Appearance | Morphological lyophilized powder |
| Storage Condition | 2-8°C |
| MDL | MFCD00131428 |
| Physical and Chemical Properties | Chemical properties kallikrein is a substance extracted from the subjawing gland or pancreas of pigs that has vasodilatory effects. White or off-white powder; Soluble in water (10%), dilute alcohol, insoluble in concentrated ethanol and general organic solvents. After being dissolved in water or normal saline, it becomes a colorless or yellowish clear solution. Ph4.5 ~ 7.8 is relatively stable. It is unstable to heat, strong acid, strong alkali, and oxidant. The isoelectric point is 3.9~4.37. |
| Use | Used as vasodilator |
kininogenin - Risk and Safety
| WGK Germany | 3 |
| RTECS | NZ2017050 |
kininogenin - Upstream Downstream Industry
kininogenin - Reference
| Reference Show more | 1. [IF=2.044] Chen Guo-Ying et al."Immobilized Kallikrein Microreactor Based on Capillary Electrophoresis for Online Enzyme Kinetics Analysis and Inhibitor Screening."Chromatographia. 2021 Oct 11 |
kininogenin - Nature
Open Data Verified Data
- This product is a substance with vasodilating effect extracted from the jawless gland or pancreas of pig, white or off-white powder; Soluble in water (10%), dilute alcohol, insoluble in concentrated ethanol and general organic solvents, soluble in water or saline into colorless or yellowish clear solution. It is unstable to heat, strong acid, strong alkali and oxidant, and is more stable at pH 4.5~7.8.
- vasopressin is an endonuclease. Unlike other enzymes, it has no effect on common protein substrates such as casein and hemoglobin, and specifically acts on the protein substrate kininogen to release kinin. It is widely found in human or mammalian tissues and secretions, in the pancreas, salivary glands, submandibular glands, intestinal wall, duodenal fluid and urine content is more abundant.
- porcine pancreatic kallikrein is a glycoprotein that contains sialic acid and is present in the gland as a zymogen. With the different content of sialic acid, l ~ 5 components can be obtained, and the removal of sialic acid does not affect the activity of the enzyme. There are two common forms, A and B, with molecular weights of 28600 and 26800, respectively, with two peptide chains, the N-terminus is isoleucine and alanine, and the c-terminus is serine and proline. Both have the same amino acid composition, containing 229 amino acid residues, but different sugar content, A containing 5. 5% sugar, B containing 11.5% sugar. The active centers of porcine pancreatic kallikrein were serine and histidine. The molecular weight of porcine kallikrein was 32000 and its isoelectric point was 3. 9-4. 37.
- kallikrein acts on kininogen to release hormone substance Kinin, tissue kallikrein hydrolyzes kininogen to release pancreatic kinin (10 peptide), blood kallikrein hydrolyzes kininogen to release bradykinin (peptide 9). It can significantly expand blood vessels, especially the expansion of skin blood vessels, but also the expansion of coronary arteries, muscles, brain and abdominal visceral blood vessels, and can improve vascular permeability, so as to play a role in regulating blood circulation. In general, the higher the purity, the worse the stability. The dried powder was stored at -20 for several months without change in activity. In water and buffer at pH = 8, it can be stored in the frozen state for a considerable period of time without inactivation. Mercapto compounds and chelating agents such as EDTA and the like can reverse the inhibition of metal ions on it. Ca2 +, Mg2 + had no effect on enzyme activity, on the contrary, high
The concentration of Ca2 +(1 mol.L-1) can increase the enzyme activity by 15% ~ 20%. Some trypsin inhibitors such as aprotinin and diisopropyl phosphate have inhibitory effects on pancreatic and submandibular gland kallikrein.
Last Update：2024-01-02 23:10:35
kininogenin - Preparation Method
Open Data Verified Data
- extraction method using porcine submandibular gland as raw material.
- extraction method using porcine pancreas as raw material.
The Fresh pig pancreas was minced, dehydrated by acetone immersion, made into pig pancreas Acetone Powder, and then 20 times the amount of 0.02 m01/L acetic acid, stirred at 10 ℃ for 12h, centrifuged, the residue was extracted with 10 times the amount of 0.02 m01/L acetic acid for 6H. The extracts were combined, then added with cold acetone to a concentration of 33%, filtered, and the filtrate was further supplemented with cold acetone to 70%, allowed to stand for 4H, centrifuged, and the precipitate was collected. The precipitate was then dehydrated and defatted with acetone and ether, and dried under vacuum to obtain the crude vasorelaxine. Add 50 times the amount of 0.2% cold sodium chloride solution to the crude vasorelaxine, adjust the pH to 8.0 with ammonia, stir and dissolve, and filter. The filtrate should be clear. The clear filtrate was cooled to 2-3 ° C. Additional cold acetone was added to reach a concentration of 40%. The centrifugal clear liquid was supplemented with acetone to a concentration of 60%, allowed to stand for 4H, and the precipitate was separated by centrifugation. The precipitate was washed with acetone and diethyl ether, and dried under vacuum to give an intermediate of vasosulfate. The intermediate was dissolved in 0.001 m01/L, pH 4.5 acetic acid buffer solution, and the precipitate was removed by centrifugation. Add the weak acid cation resin mnberliteCG50 (resin: Intermediate 50:1) into the clear solution, The resin after adsorption was washed with 0.001 m01/L, pH 4.5 buffer solution, and then eluted with 2 times 1 m01/L, ph 5.o sodium chloride solution for 1H with stirring to separate the resin. Elution of dialysis desalting, freeze-drying, that is, vaso-relaxation.
Last Update：2022-01-01 11:11:07
kininogenin - Standard
Authoritative Data Verified Data
protease extracted from porcine pancreas in this line. The activity of pancreatic kininogenase per 1 mg of protein should not be less than 300 units for oral administration or 600 units for injection.
Last Update：2024-01-02 23:10:35
kininogenin - Trait
Authoritative Data Verified Data
- This product is white or off-white powder; Odorless.
- This product is soluble in water, almost insoluble in ethanol or ether.
Last Update：2022-01-01 15:38:20
kininogenin - Introduction
Definition of enzyme activity: one unit will hydrolyze 1.0 μ mole of nα-benzoyl-l-arginine ethyl ester (BAEE) to nα-benzoyl-l-arginine and ethanol per min at pH 8.7 at 25 c.
Last Update：2022-10-16 17:29:43
kininogenin - Use
Open Data Verified Data
- vasodilator. For cerebral arteriosclerosis, occlusive endarteritis, essential hypertension, angina pectoris, occlusive Vasculitis, limbs skin ulcers, acral arterial spasm, intermittent claudication, chilblain, old limbs cold, limb sensory abnormalities and central retinitis and fundus hemorrhage.
- usage and dose of intramuscular injection, each time 10 ~ 20u> 1~3 times a day. Oral, 4~8 tablets each time, 3 times a day, fasting. Ophthalmology can also be used as subconjunctival injection, each 5u.
Last Update：2022-01-01 11:11:08
kininogenin - Differential diagnosis
Authoritative Data Verified Data
- take the appropriate amount of the product that has been measured, precision weighing, plus the purity of the phosphate buffer solution and quantitative dilution to prepare a solution containing 10 units per 1 ml. 4ml of the sample was precisely weighed, placed in a 10ml measuring flask, and diluted to a scale with the above buffer solution to serve as a test solution. Take 2.9ml of the substrate solution under the titer determination item, preheat it at 30°C ± 0.5°C for 5 minutes, put it in a 1cm Cuvette, add 0.1ml of the test solution accurately, mix well, and immediately Time, maintain the temperature in the cuvette at 30°C ± 0.5°C as determined by UV-Vis spectrophotometry (General rule 0401) at a wavelength of 253nm, 0.1mL of phosphate buffer solution in terms of purity was used instead of the test solution, and the same method was used as a blank control.
- in the chromatogram recorded under the purity 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.
Last Update：2022-01-01 15:38:21
kininogenin - Safety
Open Data Verified Data
- facial flushing, dizziness and palpitations. Occasional allergic reaction. Increased intracranial pressure, cerebral hemorrhage or other bleeding tendency is contraindicated. Malignant tumor and heart enlargement in patients with non-use.
- it was kept in a cool place and closed.
Last Update：2022-01-01 11:11:08
kininogenin - Exam
Authoritative Data Verified Data
pH
take an appropriate amount of this product, add water to dissolve and dilute the solution containing 300 units per lml, and determine it according to law (General 0631). The pH value should be 5.5~7.5.
clarity of the solution
take an appropriate amount of this product, add water to dissolve and dilute the solution containing 2mg per lml, and check according to law (General Principles 0902 first method), the solution should be clarified. (For injection)
fat
take 1.0g of this product, put it in a sealed Erlenmeyer flask, add 20ml of diethyl ether, plug it, rotate it at times, place it for about 30 minutes, pour the diethyl ether solution on the filter paper moistened with diethyl ether, the residue was filtered, and then washed with 10ml of diethyl ether. The filtrate and washing solution were combined to a constant weight evaporation dish. The diethyl ether was removed and dried at 105 ° C. For 2 hours.
purity
take an appropriate amount of this product, add mobile phase A to dissolve and dilute to prepare A solution containing about 200 units per 1 ml as A test solution; Take another pancreatic kininogenase reference substance (purity should be greater than 95%) in an appropriate amount, a solution containing about 200 units per 1 ml was prepared by the same method as a control solution. According to the high performance liquid chromatography (General 0512) test, using hydrophobic gel as filler (TSKgel Phenyl-5PW,7.5 x 75mm,10um or other suitable chromatographic column with phosphate buffer containing 1.7mol/L ammonium sulfate (pH 7.0 )(take disodium hydrogen phosphate 10.9g, sodium dihydrogen phosphate 2.3g, add water to dissolve and dilute to 1000ml, the pH value was adjusted to 50% with 7.0 phosphoric acid solution) as mobile phase A, and the above phosphate buffer solution (pH 7.0) as mobile phase B; The column temperature was 25 ° C.; The flow rate was 0.5ml per minute; the detection wavelength was 280nm. Gradient elution was performed as follows. The number of theoretical plates shall not be less than 1500 calculated by pancreatic kininogenase peak, and the degree of separation between main pancreatic kininogenase peak and adjacent impurity peak shall not be less than 0.8. 20ul of the mobile phase A, the test solution and the reference solution were injected into the liquid chromatograph respectively, and the chromatograms were recorded. The chromatograms of the test solution and the control solution were subtracted from the mobile phase A chromatogram (as A blank baseline), and baseline correction was performed. In the chromatogram of the test solution, measure the area of all chromatographic peaks after the inflection point of the blank baseline (about 16 minutes), and calculate according to the area normalization method, the area of the main peak consistent with the retention time of the main peak of the control solution shall not be less than 75% (for oral administration) or 90% (for injection).
loss on drying
taking 5.0% g of this product, using phosphorus pentoxide as desiccant, drying under reduced pressure at 60°C for 4 hours, the weight loss shall not exceed 0831 (general rule).
ignition residue
take 0.5g of this product and check it according to law (General rule 0841). The remaining residue shall not exceed 3.0%.
bacterial endotoxin
take this product, check according to law (General rule 1143), the amount of endotoxin per 1 unit of pancreatic kininogenase should be less than 2.5EU. (For injection)
Last Update：2022-01-01 15:38:22
kininogenin - Titer determination
Authoritative Data Verified Data
preparation of enzyme activity standard solution
A pancreatic kininogenase standard was taken, added with an appropriate amount of a phosphate buffer solution (pH 7.0) in terms of purity according to the indicated units to dissolve and quantitatively dilute to prepare a solution containing 10 units per 1 ml. Preparation of test solution an appropriate amount of this product is precisely weighed, and an appropriate amount of the above phosphate buffer (pH 7.0) is added to dissolve and quantitatively dilute to prepare a solution containing about 10 units per 1 ml.
preparation of substrate solution
take external benzoyl-L-Arginine ethyl ester hydrochloride 17.7mg, add Tris buffer solution (weigh Tris 12.14g, add water to dissolve, adjust pH value to 8.0 with 6mol/L hydrochloric acid solution, diluted with water to 1000ml), dissolved and diluted to 100ml, stored at 4°C.
protein content
take this product about 10mg precision weighing, according to the determination of protein content (General rule 0731 The first method) determination, that is.
specific activity
The number of units containing pancreatic kininogenase per 1 mg of protein was calculated from the measured enzyme activity and protein content.
Last Update：2022-01-01 15:38:23
kininogenin - Category
Authoritative Data Verified Data
vasodilators.
Last Update：2022-01-01 15:38:23
kininogenin - Storage
Authoritative Data Verified Data
shade, seal, and store in a cool and dry place.
Last Update：2022-01-01 15:38:23
kininogenin - Legal requirements
Authoritative Data Verified Data
This product should be extracted from Quarantine qualified pig pancreas, and the production process should comply with the requirements of the current version of "good manufacturing practice. This product for injection in the production process should adopt the appropriate Virus inactivation process.
Last Update：2022-01-01 15:38:23
kininogenin - Pancreatic Kininogenase Enteric-coated Tablets
Authoritative Data Verified Data
This product contains pancreatic kininogenase titer should not be less than 85.0% of the label.
trait
This product is an enteric-coated tablet, white or off-white after removal of the coating.
identification
In the chromatogram recorded under the purity 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
- purity take this product 5 to remove the coating, fine, weigh the appropriate amount of fine powder, put it in the centrifuge tube, add an appropriate amount of mobile phase A to dissolve and dilute pancreatic kininogenase to make A solution containing about 200 units of pancreatic kininogenase per 1 ml, mix for 2 minutes on A vortex shaker, and centrifuge (3000 revolutions per minute) for 15 minutes, take the supernatant and filter 5 and take the filtrate as the test solution; Take 1.3g of starch, 0.36g of dextrin and 0.52g of microcrystalline cellulose, put them into the centrifuge tube, add A3ml of mobile phase, and operate with the same method, take the continued filtrate as the auxiliary solution; Take the appropriate amount of pancreatic kininogenase reference substance (purity should be greater than 95%), add mobile phase A to dissolve and dilute to prepare A solution containing about 400 units per 1 ml as the reference solution; take an equal volume of The excipient solution and the reference solution, mix, as the system applicable solution. Hydrophobic gel (TSKgel Phenyl-5PW, 0512 x 75mm, 10um or other suitable chromatographic column) as tested by high performance liquid chromatography (General 7.5mm); with 1.7mol/L ammonium sulfate phosphate buffer (pH 7.0 )(take disodium hydrogen phosphate 10.9g, sodium dihydrogen phosphate 2.3g, add water to dissolve and dilute to 1000ml, adjust the pH value to 50% with 7.0 phosphoric acid solution) the solution was mobile phase A, and the temperature of the mobile phase column was 25 ° C. With the above phosphate buffer (pH 7.0); The flow rate was 0.5ml per minute; And the detection wavelength was 280nm. The linear gradient elution was performed as follows. 20ul of the mobile phase A and the applicable solution of the system were injected into the liquid chromatograph respectively, and the chromatograms were recorded. The chromatogram of the system-applicable solution was subtracted from the chromatogram of mobile phase A (as A blank baseline) and baseline corrected. The retention time of the excipient impurity peak was about 36 minutes, and the retention time of the pancreatic kininogenase peak was about 46 minutes. The number of theoretical plates shall not be less than 1500 calculated by pancreatic kininogenase peak, and the separation degree between pancreatic kininogenase peak and impurity peak of auxiliary material shall be greater than 3.0. 20ul of the test solution and the reference solution were respectively injected into the human liquid chromatograph to record the chromatogram, and the baseline correction was carried out according to the above method and the same method. In the chromatogram of the test solution, the area of each chromatographic peak after measuring the impurity peak of the auxiliary material shall be calculated by the peak area normalization method, and the area of the main peak consistent with the retention time of the main peak of the reference solution shall not be less than 70%.
- Content uniformity: Take 10 tablets of this product, remove the coating for 5 min, add appropriate amount of phosphate buffer solution (pH 7.0) under the item of purity respectively, and grind to dissolve pancreatic kininogenase, and quantitatively dilute into a solution containing 10 units of pancreatic kininogenase per 1 ml, filter, take the filtrate as the test solution, and measure according to the method under the item of potency determination of pancreatic kininogenase, comparing the potency of each tablet with the average potency of 10 tablets, the potency greater than ± 10% of the average potency shall not exceed 1 tablet and shall not exceed ± 15%; the relative standard deviation of the titer of 10 tablets should not be more than 6.0%.
- dissolution of this product, according to the dissolution and release determination method (General 0931, using the first method and the second method of enteric preparation method 2, instrument device using the third method), with 0.lmol/L hydrochloric acid solution 100ml as the dissolution medium, the speed is 75 revolutions per minute, according to the law, after 1 hour, the tablet should not have cracks, disintegration phenomenon. Discard the acid solution in each dissolution Cup, quickly rinse with water for several times, immediately add 100ml of phosphate buffer solution (pH 6.8) at the same temperature as the acid solution, continue to operate according to law, and take about 10ml of the solution after 45 minutes, filter, take the filtrate as the test solution; Take the appropriate amount of pancreatic kininogenase standard, add the above phosphate buffer (pH 6.8) according to the marked unit dissolve and quantitatively dilute to prepare a solution containing about 0.5 units (60 unit specification) or 1 unit (120 unit specification) or 2 units (240 unit specification) per 1 ml as a standard solution. Take 2 small tubes and add Tris buffer solution (weigh Tris 12.14g5, dissolve in 800ml water, adjust pH value to 8.0 with 6mol/L hydrochloric acid solution, dilute to 1000ml with water). Oml substrate solution (N-benzoyl-L-Arginine ethyl ester hydrochloride 14.14mg;(add Tris buffer 12.5ml to dissolve, store at 4°C) 0.5ml, mix well, after keeping the temperature in a water bath at 25°C ± 0.5°C for several minutes, add 0.2 of human test solution to one test tube, mix well, and immediately time, the temperature in the cuvette was maintained at 25°C ± 0.5°C, and 0.2ml phosphate buffer (pH 6.8) was added to the other test tube to replace the test solution as a blank until 1 minute, measure absorbance (A1) at the wavelength of 253mn by UV-Vis spectrophotometry (General rule 0401), and then pour the above two solutions back into the corresponding test tube, incubation was continued in a water bath at 25°C ± 0.5°C, and absorbance (A2) was measured by the same method at 16 minutes. Another standard solution was taken and operated by the same method.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
titer determination
Take 20 tablets of this product, remove the coating, precision weighing, fine grinding. Accurately weigh an appropriate amount of fine powder (about 250 equivalent to pancreatic kininogenase) in a single-position mortar, add a small amount of phosphate buffer (pH 7.0) under the purity item, and grind to dissolve pancreatic kininogenase, quantitatively transfer to a 25ml measuring flask, dilute to the scale with the above phosphate buffer (pH 7.0), shake well, filter, and take the continued filtrate as the test solution, according to the method of pancreatic kininogenase, I. E.
category
Same as pancreatic kininogenase.
specification
(1)60 units (2)120 units (3)240 units
storage
sealed and stored in a cool and dry place.
Last Update：2022-01-01 15:38:25
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Product Name: Kallikrein from porcine pancreas Visit Supplier Webpage Request for quotationCAS: 9001-01-8
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Spot supply
Product Name: Kallikrein from porcine pancreas Visit Supplier Webpage Request for quotationCAS: 9001-01-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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Raw Materials for kininogenin