CI-919 hydrate
enoxacin
CAS: 74011-58-8;84294-96-2
Molecular Formula: C30H40F2N8O9
CI-919 hydrate - Names and Identifiers
| Name | enoxacin |
| Synonyms | enoxacin Enoxacin enoxacine Enoxacin sesq CI-919 hydrate AT-2266 hydrate Enoxacin (hydrate) ENOXACIN SESQUIHYDRATE Enoxacin (Patent-No-Supply) 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic Acid 1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid sesquihydrate bis(1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-di hydro-1,8-naphthyridine-3-carboxylic acid) trihydrate C30H |
| CAS | 74011-58-8 84294-96-2 |
| InChI | InChI=1/C15H17FN4O3.H2O/c1-2-19-8-10(15(22)23)12(21)9-7-11(16)14(18-13(9)19)20-5-3-17-4-6-20;/h7-8,17H,2-6H2,1H3,(H,22,23);1H2 |
CI-919 hydrate - Physico-chemical Properties
| Molecular Formula | C30H40F2N8O9 |
| Molar Mass | 694.6836064 |
| Melting Point | 226 °C |
| Solubility | 1 M NaOH: soluble50mg/mL, clear, colorless to faintly yellow |
| Appearance | neat |
| Color | White to Off-White |
| Merck | 14,3587 |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Stability | Hygroscopic |
| Use | Broad-spectrum antibiotics, for the treatment of gram-negative and positive bacteria caused by urinary, ear, nose, throat and superficial purulent diseases and other infections |
| In vitro study | Enoxacin hydrate (Enoxacin sesquihydrate) increases siGFP-mediated gene knockdown mediated by siRNA against EGFP in HEK293 cells-based reporter system in a dose-dependent manner, with a median effective concentration (EC50) of ~30 µM, whereas it has no effect on the cells expressing GFP only. Enoxacin (50 µM) promotes the processing of miRNAs and the loading of siRNA duplexes onto RISCs in HEK293 cells. Enoxacin has no effect on the processing of pre-let-7 or pre-miR-30a by Dicer alone. However, the addition of Enoxacin can enhance the processing of let-7 or pre-miR-30a by Dicer and TRBP together. Enoxacin inhibits 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml. |
| In vivo study | Enoxacin hydrate (Enoxacin sesquihydrate; 100 µM; 2 µl; injected into ear once a day for 3 consecutive days (days 12, 13 and 14)) enhances the the GFP mRNA knockdown efficiency by Lv-siGFP (from 80% to 60%; 40% GFP mRNA level remained), whereas alone has no effect on GFP expression in GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (10 d old) with lentivirus expressing shGFP (Lv-siGFP; injected into ear for 10 days). |
CI-919 hydrate - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| HS Code | 29335990 |
CI-919 hydrate - Upstream Downstream Industry
| Raw Materials | Ethyl malonate Toluene Trichloromethane |
CI-919 hydrate - Reference
| Reference Show more | 1. [IF=2.863] Yu Zhang et al."Antibiotic residues in cattle and sheep meat and human exposure assessment in southern Xinjiang, China."Food Sci Nutr. 2021 Nov;9(11):6152-6161 |
CI-919 hydrate - Nature
Open Data Verified Data
white or light yellow-brown crystal or crystalline powder, odorless, bitter. Melting point 220-224 °c (obtained from ethanol-dichloromethane). Soluble in acetic acid, methanol-soluble, very slightly soluble in chloroform or acetone, almost insoluble in ethanol, ether or water.
Last Update：2024-01-02 23:10:35
CI-919 hydrate - Preparation Method
Open Data Verified Data
2. 6-hydroxy-5-fluoronicotinamide as raw material, by chlorination, esterification, condensation with acetylpiperazine, condensation with ethyl 3-aminopropionate, cyclization, dehydrogenation, hydrolysis product, or 2,6-= chloro-3-nitropyridine as raw material, after condensation with ethoxycarbonyl piperazine, and then ammonolysis, acetylation, reduction, diazotization, fluorination, hydrolysis, condensation with EMME (dimethyl ethoxymethylene malonate), cyclization ethylation, hydrolysis product.
Last Update：2022-01-01 09:08:48
CI-919 hydrate - Standard
Authoritative Data Verified Data
This product is 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7- (l-piperazinyl)- l, 8-naphthyridin-3-carboxylic acid sesquihydrate. The content of enoxacin (calculated as C15H17FN403) should be 98.5% to 102.0% based on the dry product.
Last Update：2024-01-02 23:10:35
CI-919 hydrate - Trait
Authoritative Data Verified Data
- This product is white to yellowish crystalline powder; Odorless.
- This product is slightly soluble in methanol, very slightly soluble in ethanol, insoluble in water; Soluble in glacial acetic acid or sodium hydroxide solution.
Last Update：2022-01-01 13:36:33
CI-919 hydrate - Use
Open Data Verified Data
quinolone broad-spectrum anti-infective drugs, the antibacterial spectrum is similar to ofloxacin, and many of the Gram-positive and negative bacteria have strong antibacterial activity. The product has not been found with the cross resistance of antibiotics, and the frequency of the emergence of natural resistant bacteria is low. It is suitable for the treatment of respiratory system infection, digestive tract infection, genitourinary system infection, skin, ear, nose, eye and throat infection, gynecological disease infection, etc.
Last Update：2022-01-01 09:08:48
CI-919 hydrate - Differential diagnosis
Authoritative Data Verified Data
- 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.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 282).
Last Update：2022-01-01 13:36:33
CI-919 hydrate - Safety
Open Data Verified Data
LD50 male and female mice, male and female rats (mg/kg): 327, 391,236,294 intravenous injection; 1237, 1320,>2000,>2000 subcutaneous injection; all> 5000 orally.
Last Update：2022-01-01 09:08:49
CI-919 hydrate - Exam
Authoritative Data Verified Data
clarity and color of solution
take 0.5g of this product, and add 10ml of sodium hydroxide solution to dissolve. The solution should be clear and colorless. If it is turbid, it should not be more concentrated compared with No. 1 turbidity standard solution (General rule 0902 first method); in case of color development, it shall not be deeper in comparison with the yellow or yellow-green standard colorimetric solution No. 4 (general principles 0901, Method 1).
Related substances
take about 25mg of this product, put it in a 100ml measuring flask, add 0. About 20ml of 1 mol/L hydrochloric acid solution was dissolved, diluted to the scale with mobile phase A, and then shaken to be used as A test solution; 1ml was accurately measured and placed in A lOOml measuring flask, the mixture was diluted to the scale with mobile phase A, shaken well, and as A control solution, measured by high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as A filler; 0.025mol/L phosphoric acid solution (adjusted to pH 3.0 with triethylamine)-fermentation-acetonitrile (80:10:10) as mobile phase A; using 0.025mol/L phosphoric acid solution (with triethylamine to adjust the pH value to 3.0)-methanol-acetonitrile (350:325:325) as mobile Phase B, column temperature is 40°C, the detection wavelength was 269nm. Linear gradient elution was carried out according to the following table, and an appropriate amount of enoxacin control, norfloxacin impurity B control and ofloxacin control was added. 1 mol/ L hydrochloric acid solution was dissolved and diluted to prepare a mixed solution containing enoxacin (calculated as C15H17FN403) 0.25mg, norfloxacin impurity B 2.5ug and ofloxacin 2.5ug per 1 ml, the chromatogram showed that the retention time of enoxacin peak was about 9 minutes. The separation degree of norfloxacin impurity B peak and enoxacin peak should be greater than 4.9, and the separation degree of enoxacin peak and ofloxacin peak should be greater than 1.1. Accurately take 20 u1 of the test solution and the control solution, respectively inject human liquid chromatograph, record the chromatogram, if there are impurity peaks in the chromatogram of the test solution, the single impurity peak area shall not be greater than 0.3 times (0.3%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%). The peaks in the chromatogram of the test solution which were 0.05 times smaller than the main peak area of the control solution were ignored.
loss on drying
take this product, dry to constant weight at 105°C, weight loss should be 7.8% ~ 9.0% (General 0831).
ignition residue
take l.Og of this product, put it in a platinum crucible, 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 13:36:34
CI-919 hydrate - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with eighteen alkyl silane was used as filler; 0.025mol/L phosphoric acid solution (adjusted to pH 3.0 with triethylamine)-methanol-acetonitrile (80:10:10) as mobile phase; the detection wavelength was 269nm, and 5mg of enoxacin control, 2.5mg of norfloxacin impurity B control, and mg of ofloxacin control, respectively. 1 mol/L hydrochloric acid solution about 4ml to dissolve, dilute to the scale with mobile phase, shake, take 20ul injection liquid chromatograph, record chromatogram, enoxacin peak retention time is about 9 minutes, the resolution of norfloxacin impurity B peak and enoxacin peak should be greater than 4.9, and the resolution of enoxapari peak and ofloxacin peak should be greater than 1.1.
assay
take this product about 25mg, precision weighing, 100ml flask, add 0.1 mol/L hydrochloric acid solution about 20ml to dissolve, dilute to scale with mobile phase, shake well, take 5ml with precision, put in 25ml measuring flask, dilute to scale with mobile phase, shake well, as the sample solution, the 20u1 was injected into the human liquid chromatograph accurately, and the chromatogram was recorded. An appropriate amount of the reference substance of enoxacin was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 13:36:35
CI-919 hydrate - Category
Authoritative Data Verified Data
quinolones.
Last Update：2022-01-01 13:36:35
CI-919 hydrate - Storage
Authoritative Data Verified Data
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:36:35
CI-919 hydrate - Enoxacin tablets
Authoritative Data Verified Data
This product contains enoxacin (C15H17FN4O3) should be 93.0% to 107.0% of the label amount.
trait
This product is white-like or yellowish or film-coated tablets, white or yellowish after removing the coating.
identification
- 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.
- take an appropriate amount of fine powder of this product and add 0.1 mol/ L sodium hydroxide solution is dissolved and diluted to make a solution containing about 4ug of enoxacin (calculated as C15H17FN403) per 1 ml, filtered and determined by UV-Vis spectrophotometry (General rule 0401), there is maximum absorption at wavelengths of 266nm and 346nm.
examination
- Related substances take an appropriate amount of fine powder of this product (about equivalent to enoxacin, 25mg based on C15H17FN403), weigh it accurately, put it in a 100ml measuring flask, add 0. About 20ml of 1 mol/L hydrochloric acid solution to dissolve enoxacin, dilute to the scale with mobile phase A, shake, filter, and take the continued filtrate as the test solution, the single impurity peak area shall not be greater than 0.4 times (0.4%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 second method), water 900ml as the dissolution medium, the speed of 50 rpm, according to the law, after 45 minutes, take the appropriate amount of solution, filtration, precision amount of filtrate, with hydrochloric acid solution (dilute hydrochloric acid 24ml add water to 1000ml) A solution containing about 4ug of enoxacin (C15H17FN403) per 1 ml was prepared by quantitative dilution, and the absorbance was measured at the wavelength of 268mn by ultraviolet-visible spectrophotometry (General rule 0401); another appropriate amount of enoxacin reference substance was carefully weighed, and the above hydrochloric acid solution was added to dissolve and quantitatively dilute to make a solution containing about 4ug per 1 ml, which was determined 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 10 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (equivalent to enoxacin, according to C15H17FN403 0.lg), put in 200ml measuring flask, add 0.1 mol/ L hydrochloric acid solution about 80ml to dissolve, diluted with mobile phase to scale, shake well, filter, Take 5ml of filtrate accurately, put it in 50ml measuring flask, dilute with mobile phase to scale, shake, as a test solution, according to the method under the item of enoxacin measurement, obtained.
category
same with enoxacin.
specification
calculated as C15H17FN403 (1)0.lg (2)0.2g
storage
light shielding, sealed storage.
Last Update：2022-01-01 13:36:36
CI-919 hydrate - Enoxacin cream
Authoritative Data Verified Data
This product contains enoxacin (C15H17FN403) should be 90.0% to 110.0% of the label amount.
trait
This product is white to light yellow cream.
identification
- 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.
- take an appropriate amount of this product, add 0. An appropriate amount of 1 mol/ L sodium hydroxide solution is heated in a water bath at 50-60 ℃ and diluted to make a solution containing 4ug of enoxacin (calculated as C15H17FN403) per 1 ml, which is cooled in an ice bath, the substrate was coagulated, filtered, and had an absorption maximum at wavelengths of 266nm and 0401 nm as determined by UV-Vis spectrophotometry (general).
examination
should comply with the relevant provisions under Cream (General rule 0109).
Content determination
take an appropriate amount of this product (about equivalent to enoxacin, 25mg according to C15H17FN403), weigh it accurately, put it in a 100ml beaker, add 0.1 mol/ L hydrochloric acid solution about 50ml, stirred evenly, so that enoxacin dissolved, transferred to a 100ml measuring flask, diluted with methanol to the scale, shake, filter, precision take filtrate 5ml, set in a 25ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, and measure according to the method of enoxacin.
category
same with enoxacin.
specification
10G: 0.1g (calculated as C15H17FN403)
storage
sealed and stored in a cool and dry place.
Last Update：2022-01-01 13:36:37
CI-919 hydrate - Enoxacin Capsules
Authoritative Data Verified Data
This product contains enoxacin (C15H17FN403) should be 90.0% to 110.0% of the label amount.
trait
The contents of this product are white to yellowish powder or granules.
identification
- 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 control solution.
- take an appropriate amount of the contents of this product and add O. 1 mol/ L sodium hydroxide solution is dissolved and diluted to make a solution containing about 4ug of enoxacin (calculated as C15H17FN403) per 1 ml, filtered and determined by UV-Vis spectrophotometry (General rule 0401), there is maximum absorption at wavelengths of 266nm and 346nm.
examination
- Related substances take an appropriate amount of the contents of this product (about equivalent to enoxacin, 25mg as per C15H17FN403), weigh it accurately, put it in a 100ml measuring flask, add 0. About 20ml of 1 mol/L hydrochloric acid solution was used to dissolve enoxacin, and the solution was diluted with mobile phase A to the scale. The solution was filtered by shaking and the filtrate was continued as the test solution, the single impurity peak area shall not be greater than 0.4 times (0.4%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- dissolution dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), with dilute hydrochloric acid solution (dilute hydrochloric acid 24ml and water to 1000ml) 900ml as the dissolution medium, the rotation speed is 100 rpm, and the operation is carried out according to law. After 30 minutes, the appropriate amount of the solution is taken, filtered, and the appropriate amount of the filtrate is taken, A solution containing about 4ug of enoxacin (C15H17FN403) per 1 ml was prepared by quantitative dilution with dissolution medium, and the absorbance was determined by UV-Vis spectrophotometry (General rule 0401) at the wavelength of 268mn; in addition, an appropriate amount of enoxacin reference substance was accurately weighed, dissolved and quantitatively diluted with dissolution medium to make a solution containing about 4ug per 1 ml, and the dissolution amount of each particle was calculated by the same method. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
take the contents under the item of difference in loading, mix evenly, grind finely, weigh an appropriate amount (about 0.lg equivalent to enoxacin, calculated as C15H17FN403), put it in a 200ml measuring flask, and add 0.1 mol/L hydrochloric acid solution about 80ml to dissolve, diluted with mobile phase to scale, shake well, filter, Take 5ml of filtrate accurately, put it in 50ml measuring flask, dilute with mobile phase to scale, shake, as a test solution, according to the method under the item of enoxacin measurement, obtained.
category
same with enoxacin.
specification
calculated as C15H17FN403 (l)0.1g (2)0.2g
storage
light-shielded, sealed, and stored in a dry place.
Last Update：2022-01-01 13:36:38
CI-919 hydrate - Enoxacin Eye Drops
Authoritative Data Verified Data
This product contains enoxacin (C15H17FN403) should be 90.0% to 110.0% of the label amount.
trait
This product is colorless to yellowish clear liquid.
identification
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be the retention time of the main peak of the reference solution Consistent.
- take an appropriate amount of this product, add 0.1 mol/L sodium hydroxide solution is prepared to contain enoxacin (C15H17FN403) 4ug per l of solution, according to UV-visible spectrophotometry (General 0401) determination, there is maximum absorption at wavelengths of 266nm and 346nm.
examination
- the pH value should be 4.5 to 5.5 (General 0631).
- the color of this product, compared with the yellow or yellow-green No. 2 Standard Colorimetric liquid (General Principles 0901 first method), shall not be deeper.
- Related Substances: take 2ml of this product, put it in A 25ml measuring flask, dilute it to the scale with mobile phase A, shake it, and use it as A test solution, if there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.4 times (0.4%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
- others shall comply with the relevant provisions under Ophthalmic Preparations (General rule 0105).
Content determination
take 2ml of this product with precision, put it in a 25ml measuring flask, dilute it to the scale with mobile phase, shake it well, take 5ml with precision, put it in a 25ml measuring flask, dilute it to the scale with mobile phase, shake, as a test solution, according to the method under the item of enoxacin measurement, obtained.
category
same with enoxacin.
specification
8ml:24mg (based on C15H17FN403)
storage
shade, seal, and store in a cool place.
Last Update：2022-01-01 13:36:39
Supplier List
Spot supply
Product Name: Enoxacin Hydrate Visit Supplier Webpage Request for quotationCAS: 84294-96-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Enoxacin sesquihydrate Visit Supplier Webpage Request for quotationCAS: 84294-96-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Enoxacin Hydrate Visit Supplier Webpage Request for quotationCAS: 84294-96-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Enoxacin sesquihydrate Visit Supplier Webpage Request for quotationCAS: 84294-96-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
Raw Materials for CI-919 hydrate