3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE
amiloride hydrochloride hydrate
CAS: 2016-88-8
Molecular Formula: C6H8ClN7O.ClH
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Names and Identifiers
| Name | amiloride hydrochloride hydrate |
| Synonyms | amiprazidine Amiloride HCl amiloridechloride HCL AMILORIDE HCL Amiloride Hydrochloride Amipramidin hydrochloride Amipramizide hydrochloride amiloride hydrochloride hydrate n-amidino-3,5-diamino-6-chloro-pyrazinecarboxamidmonohydrochloride N-amidino-3,5-diamino-6-chloropyrazinecarboxamide monohydrochloride 3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE (3,5-diamino-6-chloropyrazin-2-yl)-N-(diaminomethylidene)oxomethanaminium |
| CAS | 2016-88-8 |
| EINECS | 217-958-2 |
| InChI | InChI=1/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)/p+1 |
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C6H8ClN7O.ClH |
| Molar Mass | 266.09 |
| Melting Point | 293-294°C |
| Boling Point | 628.1°C at 760 mmHg |
| Flash Point | 333.7°C |
| Water Solubility | <0.1 g/100 mL at 19.5 ºC |
| Solubility | H2O: 50mg/mL, clear, yellow-green |
| Vapor Presure | 1.08E-15mmHg at 25°C |
| Appearance | powder |
| Color | yellow |
| Storage Condition | Store at RT |
| Physical and Chemical Properties | Yellow or greenish-yellow powder. Melting point 293.5 °c. Soluble in water, almost odorless, amiloride [2609-46-3] melting point, 240.5-241.5 ℃. |
| Use | Used as a weak diuretic |
| In vitro study | Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC), with IC 50 ranging from 0.1 μm to 0.5 μm. Amiloride is a relatively poor Na / H Exchanger (NHE) inhibitor, with IC50 as low as 3 μm at low external sodium ion concentrations and as high as 1 mM at high external sodium ion concentrations. Amiloride is a weak inhibitor of Na / Ca 2 Exchange (NCX) with IC 50 of 1 mM. Amiloride(1 μm) and Benzamil(30 nM) inhibit vasoconstriction, inhibiting myogenesis in response to increased perfusion pressure by blocking the activity of the ENaC protein. In vascular smooth muscle cells (VSMC), Amiloride completely inhibits sodium influx. |
| In vivo study | In DOCA salt hypertensive rats, Amiloride(1 mg/kg/day, subcutaneously) reversed the increase in initial collagen deposition and prevented further increases. In saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP), Amiloride delays the onset of proteinuria and improves brain and kidney histological scores. Compared with the control group. In hypertensive salt-dependent animals, Amiloride antagonizes or prevents the effects of aldosterone in these cells and in vascular and renal tissues. |
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Risk and Safety
| Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | UQ2275500 |
| HS Code | 29339980 |
| Hazard Class | 6.1(a) |
| Packing Group | II |
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Reference
| Reference Show more | 1. [IF=6.988] Yingying Song et al."Photoresponsive Polypeptide-Glycosylated Dendron Amphiphiles: UV-Triggered Polymersomes, OVA Release, and In Vitro Enhanced Uptake and Immune Response."Biomacromolecules. 2020;21(12):5345–5357 2. [IF=6.953] Hongdong Song et al."Fabrication of chitosan-coated epigallocatechin-3-gallate (EGCG)-hordein nanoparticles and their transcellular permeability in Caco-2/HT29 cocultures."Int J Biol Macromol. 2021 Dec;: |
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Standard
Authoritative Data Verified Data
This product is n-amidino-3, 5-diamino-6-chloropyrazine-2-carboxamide hydrochloride dihydrate. The content of C6H8C1N70 • HCl shall not be less than 98.5% calculated as anhydrous.
Last Update：2024-01-02 23:10:35
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Trait
Authoritative Data Verified Data
- This product is light yellow or yellow-green powder; Odorless or almost odorless.
- This product is slightly soluble in water, very slightly soluble in ethanol, and almost insoluble in chloroform or ether.
Last Update：2022-01-01 15:05:11
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.758 ml | 18.791 ml | 37.581 ml |
| 5 mM | 0.752 ml | 3.758 ml | 7.516 ml |
| 10 mM | 0.376 ml | 1.879 ml | 3.758 ml |
| 5 mM | 0.075 ml | 0.376 ml | 0.752 ml |
Last Update：2024-01-02 23:10:35
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Differential diagnosis
Authoritative Data Verified Data
- take this product, add 0.1 mol/ L hydrochloric acid solution was dissolved and diluted to prepare a solution containing about 10ug per 1 ml, which was determined by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at a wavelength of 285nm and 362nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 828).
- take about 20mg of this product, add 20ml of water to dissolve, Dropwise add excess nitric acid to complete precipitation, filter, filtrate chloride to identify (1) reaction (General 0301).
Last Update：2022-01-01 15:05:11
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Exam
Authoritative Data Verified Data
acidity
take 0.10g of this product, add 20ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 3.8~5.2.
Related substances
take this product, add methanol to dissolve and dilute to make a solution containing about 2mg per 1 ml as a test solution; Take another 3,5-diamino-6-chloropyrazine-2-carboxylic acid methyl ester (impurity I) reference substance, precision weighing, respectively, plus methanol dissolved and quantitatively diluted to make each 1 mL solution containing about 10ug and 4ug, as Control Solutions (1) and (2). According to the thin layer chromatography (General 0502) test, absorb the above three solutions of each L01, respectively, on the same silica gel G thin layer plate, with dioxane-dilute ammonia solution-water (90:6:6) for the development of the agent, expand, dry, set the UV light (365nm) under the view. If the test solution shows impurity spots corresponding to the reference solution (1), the fluorescence intensity of the test solution should not be stronger than that of the main spot of the reference solution (1); If other impurity spots are shown, the main spot should not be stronger than the control solution (2).
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 11.0% ~ 13.0%.
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 15:05:12
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Content determination
Authoritative Data Verified Data
take this product about 0.2g, precision weighing, plus O.Olmol/L hydrochloric acid solution 5ml and ethanol 50ml to dissolve, according to the potentiometric titration method (General 0701), with sodium hydroxide titration solution (0.1 mol/L) titration, the difference between the two burst point volumes as The titration volume. Each 1 ml of sodium hydroxide titration solution (0.1 mol/L) corresponds to 26.61mg of C6H8C1N70. HCl.
Last Update：2022-01-01 15:05:12
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Category
Authoritative Data Verified Data
diuretics.
Last Update：2022-01-01 15:05:13
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 15:05:13
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Compound Amiloride Hydrochloride Tablets
Authoritative Data Verified Data
This product contains amiloride hydrochloride (according to C6H8C1N70 • HC1) and hydrochlorothiazide (C7H8C1N04S2) should be 90.0% ~ 110.0% of the label amount.
prescription
amiloride hydrochloride 2.5G
Hydrogen thiazoles 25g
Made into 1000 tablets
trait
This product is white-like to yellowish.
identification
In the chromatogram recorded under the content determination item, the retention time of the two main peaks of the test solution should be consistent with the retention time of the corresponding two main peaks in the control solution.
examination
- 4-amino-6-chlorobenzene-1, 3-disulfonamide: take the sample solution under the content determination item as the sample solution; Take 1ml for precision measurement, set it in a 100ml measuring flask, dilute it to the scale with mobile phase, shake it well, and use it as a control solution, hydrochlorothiazide control and amiloride hydrochloride control were dissolved and diluted with mobile phase to prepare each containing 0. The solution of lmg is used as the applicable solution of the system, and the detection wavelength is 265nm according to the chromatographic conditions under the content determination item. 20u1 is injected into the liquid chromatograph, and the number of theoretical plates is not less than 1500 based on the hydrogen thiazide peak, the degree of separation of the 4-amino -6-chlorobenzene -1, 3-disulfonamide peak, hydrogen thiazide peak and amiloride peak shall meet the requirements. 20 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, record the chromatogram ^ If there is a peak in the chromatogram of the test solution that is consistent with the retention time of the peak of 4-amino-6-chlorobenzene-1, 3-disulfonamide in the solution for which the system is applicable, the peak area shall not be greater than the hydrogen thiazide peak area in the control solution (1.0%).
- 1 tablet of this product was placed in a 25ml measuring flask, with 7.5ml methanol and O. 1 mol/L hydrochloric acid solution 1ml, according to the method under the content determination item, from the "ultrasonic treatment", according to the law, shall comply with the provisions (General Principles 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.100 ml of 1 mol/ L hydrochloric acid solution is the dissolution medium, and the rotation speed is revolutions per minute. The operation is carried out according to law. After 30 minutes, 20ml of the solution is taken, filtered, and the filtrate is taken for standby.
- amiloride hydrochloride take the above solution, according to UV-visible spectrophotometry (General rule 0401), determine the absorbance at the wavelength of 365nm; Take the reference substance of amiloride hydrochloride, add 0.1 mol/ L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 2.5ug per 1 ml, which was measured by the same method, and the dissolution amount of each tablet was calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- 5ml of the above solution was accurately measured for hydrochlorothiazide, placed in a 50ml measuring flask, and used O. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, and measure the absorbance at the wavelength of 272mn by UV-Vis spectrophotometry (General rule 0401), precision weighing, add 0.1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 2.5ug per 1 ml, and the absorbance was measured by the same method to calculate the dissolution amount of each tablet. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
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; Phosphate buffer solution (take potassium dihydrogen phosphate 13.6g, add water 80ml to dissolve, adjust pH to 3.0 with phosphoric acid, diluted to 100ml with water)-methanol-water (4:25:71) as mobile phase; Detection wavelength was 286NM. The number of theoretical plates shall not be less than 1000 calculated by amiloride peak, and the separation degree between amiloride peak and chlorazin peak shall meet the requirements.
- determination of 10 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount of [approximately equivalent to 5mg of minolili hydrochloride (as per C6H8ClN7O • HC1)], put it in a 50ml measuring flask, add 15ml methanol and 0.1 mol/L hydrochloric acid solution 2ml, ultrasonic dissolution of amiloride hydrochloride and hydrochlorothiazide, cold, diluted with water to the scale, shake, filter, take the filtrate as a test solution, take 10u1 injection liquid chromatograph accurately, record chromatogram; Take about 100mg of hydrochlorothiazide reference substance, weigh it accurately, put it in 100ml measuring flask, add 20ml methanol to dissolve it, precision Add amiloride hydrochloride control solution (take amiloride hydrochloride control, precision weighing, and methanol dissolved and quantitatively diluted to make a solution containing about 1 mg per 1 ml) 10ml, plus O.lmol/L hydrochloric acid solution 4ml, diluted with water to the scale, shake, the same method. According to the external standard method to calculate the peak area, that is.
category
diuretics.
storage
light shielding, sealed storage.
Last Update：2022-01-01 13:43:32
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Amiloride Hydrochloride Tablets
Authoritative Data Verified Data
This product contains amiloride hydrochloride according to C6H8C1N70 • HCl, should be 90.0% ~ 110.0% of the label amount.
trait
This product is a light yellow tablet.
identification
- take an appropriate amount of fine powder of this product and add O. 1 mol/L hydrochloric acid solution is dissolved and diluted to make a solution containing about 10ug of amiloride hydrochloride in 1 ml, filtered, and the filtrate is determined by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at a wavelength of 285nm and 362nm.
- take an appropriate amount of the fine powder of this product (about 5mg of amiloride hydrochloride), add 25ml of methanol, shake to dissolve amiloride hydrochloride, filter, and take the filtrate as the test solution; an additional amiloride hydrochloride control was dissolved in methanol and diluted to prepare a solution containing about 0.2mg per 1 ml as a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of each L01, respectively, on the same silica gel H thin layer plate, with dioxane-dilute ammonia solution-water (90:6:6) for the development of the agent, expand, dry, set the UV light (365nm) under the inspection. The position and fluorescence intensity of the main spot displayed by the test solution should be the same as that of the control solution.
examination
- Content uniformity take 1 tablet of this product, put it in a 50ml measuring flask, and determine it according to the method under the content determination item. It shall comply with the regulations (General rule 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.900ml of 1 mol/L hydrochloric acid solution is the dissolution medium, and the rotation speed is 50 revolutions per minute, which is operated according to law. After 30 minutes, 10ml of the solution is taken, filtered, and the filtrate is taken, according to UV-visible spectrophotometry (General rule 0401), the absorbance was measured at the wavelength of 362nm; Another amiloride hydrochloride reference substance, precision weighing, plus O. 1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 2.5ug per 1 ml, which was measured by the same method, and the dissolution amount of each tablet was calculated. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount [about equivalent to amiloride hydrochloride (according to C6H8C1N70 • HCl) 5mg], put in 100ml measuring flask, add 0.60ml of 1 mol/L hydrochloric acid solution was placed in a water bath for about 30 minutes and shaken constantly to dissolve amiloride hydrochloride, let it cool, and use O. 1 mol/L hydrochloric acid solution diluted to the scale, shake, immediately take the appropriate amount, put the plug in the centrifuge tube, centrifuge, take the supernatant 5ml, put the 25ml flask, use 0. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, and measure the absorbance at the wavelength of 362nm by UV-Vis spectrophotometry (General rule 0401), precision weighing, add 0.lmol/L hydrochloric acid solution is dissolved and quantitatively diluted to make a solution containing about 10ug per lml, which is determined and calculated by the same method.
category
Same as amiloride hydrochloride.
specification
2.5mg (calculated as C6H8C1N70 • HCl)
storage
light shielding, sealed storage.
Last Update：2022-01-01 15:05:14
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| biological activity | Amiloride (MK-870) is a selective T-type calcium channel blocker, epithelial sodium channel(ENaC) blocker, urokinase plasminogen activator (uPA) inhibitor, Ki = 7 μM. |
| Target | Value |
| Sodium channel | |
| T-type calcium channel | |
| uPA | 7 μM(Ki) |
| use | is a weak diuretic. The effect is similar to that of aminobenzene, and it is currently the strongest drug among sodium steroidal potassium diuretics. used as weak diuretic |
Last Update：2024-04-09 20:52:54
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Product Name: AMiloride Hydrocholride Visit Supplier Webpage Request for quotationCAS: 2016-88-8
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Product Name: Amiloride Hydrochloride Request for quotation
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: AMiloride Hydrocholride Visit Supplier Webpage Request for quotationCAS: 2016-88-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
3,5-DIAMINO-N-(AMINOMETHYL)-6-CHLOROPYRAZINE CARBOXAMIDE HYDROCHLORIDE
3,3,3-三氟丙胺
Methyl glucoside propoxylate
4-NITRO-PYRIDIN-3-YLAMINE
1-甲基-4-氨基-3-丙基吡唑-5-甲酰胺
3-Butoxy Propylamine
2-硝基-9,9-二苯基-9H-芴
3-氯-异氰酸对氟苯基酯
3,3,3-三氟丙胺
Methyl glucoside propoxylate
4-NITRO-PYRIDIN-3-YLAMINE
1-甲基-4-氨基-3-丙基吡唑-5-甲酰胺
3-Butoxy Propylamine
2-硝基-9,9-二苯基-9H-芴
3-氯-异氰酸对氟苯基酯