6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL)
Cilostazol
CAS: 73963-72-1
Molecular Formula: C20H27N5O2
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Names and Identifiers
| Name | Cilostazol |
| Synonyms | Cilostazol Cilostazole CILOSTAZOL JP 6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE 6-[4-(1-cyclohexyl-1h-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1h)-quinolinone 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one 6-[4-(1-cyclohexyl-5-tetrazolyl)butoxy]-1,2,3,4-tetrahydro-2-oxoquinolinone 6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) OPC-13013, Pletal, 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone OPC 13013, OPC 21, Pletaal, 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone |
| CAS | 73963-72-1 |
| EINECS | 689-122-9 |
| InChI | InChI=1/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26) |
| InChIKey | RRGUKTPIGVIEKM-UHFFFAOYSA-N |
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Physico-chemical Properties
| Molecular Formula | C20H27N5O2 |
| Molar Mass | 369.46 |
| Density | 1.1832 (rough estimate) |
| Melting Point | 159-160°C |
| Boling Point | 499.57°C (rough estimate) |
| Flash Point | 355.8°C |
| Solubility | DMSO 74 mg/mL Water <1 mg/mL Ethanol 6 mg/mL |
| Vapor Presure | 1.56E-17mmHg at 25°C |
| Appearance | solid |
| Color | off-white |
| Maximum wavelength(λmax) | ['257nm(MeOH)(lit.)'] |
| Merck | 14,2277 |
| pKa | 14.22±0.20(Predicted) |
| Storage Condition | Inert atmosphere,Room Temperature |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months |
| Refractive Index | 1.7600 (estimate) |
| MDL | MFCD00866780 |
| Physical and Chemical Properties | Colorless needle-like crystals were obtained from methanol with a melting point of 159.4-160.3 °c. UV absorption maximum (methanol):257nm (η15200). Soluble in acetic acid, chloroform, n-methyl-2-pyrrolidone or dimethyl sulfoxide, a few insoluble in ether, water, 0.1mol/L hydrochloric acid or 0.1mol/L sodium hydroxide. |
| Use | Triphosphodiesterase (PDE 3) inhibitor,. Antithrombotic and cardiotonic agents |
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| WGK Germany | 2 |
| RTECS | VC8277500 |
| HS Code | 29339900 |
| Toxicity | LD50 in mice, rats (mg/kg): >2000, >2000 i.p.; >5000, >5000 orally (Nomura) |
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Nature
Open Data Verified Data
colorless needle-like crystals were obtained from methanol, melting point 159. 4-160,3 °c. UV absorption maximum (methanol):257nm(e:15200). Soluble in acetic acid, chloroform, n-methyl-2-pyrrolidone or dimethyl sulfoxide, almost insoluble in ether, water, 0. 1mol/L hydrochloric acid or 0.1 mol/L sodium hydroxide.
Last Update：2024-01-02 23:10:35
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Preparation Method
Open Data Verified Data
phosphorus pentachloride was slowly added to a benzene solution of 5-chloro-n-cyclohexylvaleramide under ice-cooling, and a benzene solution of ammonia was added under stirring at room temperature. The reaction was stirred and worked up to give 5-(4-chlorobutyl)-1-cyclohexyltetrazole. 6 a hydroxyl group of 3.4 a two hydrogen 2 (1H)-quinoline ketone and potassium hydroxide dissolved in isopropanol, under reflux, drop add 5 (4-chlorine butyl)-1-cyclohexyltetrazole in isopropanol. Reflux stirring was continued and the resulting material was treated as cilostazol.
Last Update：2022-01-01 09:23:47
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Standard
Authoritative Data Verified Data
This product is 6-4 (1-cyclohexyl-h-tetrazol-5-yl) butoxy]-3, 4-dihydroquinolone. The content of C24H27N502 shall be 98.0% ~ 102.0% calculated as dry product.
Last Update：2024-01-02 23:10:35
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is soluble in glacial acetic acid or chloroform, dissolved in N,N-dimethylformamide, slightly soluble in methanol or anhydrous ethanol, in water, 0.1 mol/L hydrochloric acid solution or 0. Almost insoluble in 1 mol/L sodium hydroxide solution.
melting point
The melting point of this product (General 0612) is 157~161°C.
Last Update：2022-01-01 11:44:23
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Use
Open Data Verified Data
developed by Otsuka Pharmaceutical Company, Japan, launched in 1988. It has vasodilator effect and antiplatelet function, and increases the concentration of cAMP in platelets and smooth muscle by inhibiting the activity of phosphodiesterase in platelets and vascular smooth muscle, and exerts antiplatelet effect and vasodilator effect. Inhibition of ADP, epinephrine, collagen and arachidonic acid-induced platelet aggregation and release in the early and second phase, the model of cerebral circulation and peripheral circulation disorder caused by sodium laurate has obvious antithrombotic effect. It can be used to treat chronic arterial occlusive disease caused by atherosclerosis, Takayasu arteritis, Thromboangiitis obliterans, diabetes, etc.
Last Update：2022-01-01 09:23:48
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - 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 754).
Last Update：2022-01-01 11:44:23
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Safety
Open Data Verified Data
mouse, rat LDso( mg/kg):>2000.>2000 intraperitoneal injection;>5000,>5000 orally.
Last Update：2022-01-01 09:23:48
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Exam
Authoritative Data Verified Data
Related substances
take this product, add methanol-water (70:30) to dissolve and dilute to prepare a solution containing about 0.25mg of cilostazol per 1 ml as a test solution; Take lml for precision measurement, in a 100ml measuring flask, dilute to the mark with methanol-water (70:30) and shake to a control solution. According to the method under the content determination item, 20 u1 of the test solution and the control solution are respectively injected into the human liquid chromatograph, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If the impurity peak is shown in the chromatogram of the test solution, the sum of the peak areas of each impurity shall not be greater than the main peak area of the control solution (1.0%).
residual solvent
take this product, precision weighing, plus N,N-dimethylformamide dissolved and quantitatively diluted into a solution containing about 75mg per 1 ml, as a test solution; Take toluene, dichloromethane, acetone and ethanol, precision weighing, and quantitative dilution of N,N-dimethylformamide to make a mixed solution containing about 66.8ug, 45ug, 375ug and 375ug per lml, respectively, as a control solution. Take 4ml of reference solution and 4ml of test solution respectively, put them in 20ml headspace bottles, then add 6.0ml of water respectively, shake well, and seal immediately, test as residual solvent assay (General 0861 second method). A quartz capillary column with 5% phenyl-95% methyl polysiloxane (or similar polar) as the stationary liquid is used as the column; The starting temperature is 35°C, the temperature is maintained for 7 minutes, and the temperature is raised to 220°C at a rate of 25°C per minute, it was maintained for 5 minutes; The inlet temperature was 130°C; The detector temperature was 250°C; The headspace bottle equilibrium temperature was 80°C and the equilibrium time was 60 minutes. Take the headspace injection of the reference solution, and the separation degree between the peaks of each component shall meet the requirements; The number of theoretical plates shall not be less than 7000 based on the ethanol peak. The test solution and the reference solution were respectively injected in the headspace, and the chromatograms were recorded. The residual amounts of toluene, dichloromethane, acetone and ethanol were calculated by the peak area according to the external standard method.
chloride
take 0.50g of this product, add 50ml of water, put it on a water bath and heat it for 10 minutes, shake it from time to time, let it cool, filter it, take 25ml of filtrate, and check it according to law (General rule 0801), with standard sodium chloride solution 7.0ml of the control solution should not be more concentrated (0.028%).
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
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 11:44:24
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - 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 A filler; Water was used as mobile phase A, methanol was used as mobile Phase B, and gradient elution was carried out according to the following table; The detection wavelength was 257nm. The number of theoretical plates is not less than 5000 based on the cilostazol peak.
assay
take this product about 20mg, precision weighing, 200ml flask, add methanol-water (70:30) appropriate amount, ultrasonic dissolution, with methanol-water (70:30) dilute to the scale, shake, as a test solution, take the precision of 20u1 injection of human liquid chromatography, record the chromatogram; Another cilostazol reference substance, the same method for determination. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:44:25
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Category
Authoritative Data Verified Data
Anti-platelet aggregation drugs.
Last Update：2022-01-01 11:44:25
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Storage
Authoritative Data Verified Data
sealed storage.
Last Update：2022-01-01 11:44:25
6-[4-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL)BUTOXY]-3,4-DIHYDRO-2(1H)-QUINOLINONE(CILOSTAZOL) - Cilostazol capsules
Authoritative Data Verified Data
This product contains Cilostazol (C24H27N502) should be labeled the amount of 90.0% ~ 110.0%.
trait
The content of this product is white or white particles or powder.
identification
- the sample solution under the content measurement item was taken and measured by ultraviolet-visible spectrophotometry (General rule 0401), and there was a maximum absorption at a wavelength of Nm.
- take the test solution under the item of related substances as the test solution, and take the cilostazol reference substance, add the mobile phase to dissolve and dilute to prepare a solution containing 0.25mg of cilostazol per 1 ml, as a control solution. 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 according to the chromatographic conditions under the relevant substances.
examination
- relevant substances: take an appropriate amount of the fine powder of this product (about 12.5mg equivalent to cilostazol), weigh it accurately, put it in a 50ml measuring flask, use 19ML of acetonitrile, and sonicate it for 10 minutes to dissolve cilostazol, add 0.07moll/L phosphoric acid solution (adjust the pH value to 2.5 with triethylamine) to the scale, shake well, filter, and take the continued filtrate as the test solution, set in a 100ml measuring flask, dilute to the scale with the mobile phase, and shake to serve as a control solution. According to the test of high performance liquid chromatography (General 0512), silica gel bonded with eighteen alkyl silane as filler; 0.07mol/ L phosphoric acid solution (adjusted to pH 2.5 with triethylamine)-ethylene (62:38) as mobile phase; The detection wavelength was 257mn. The number of theoretical plates shall not be less than 2000 calculated by cilostazol peak, and the separation degree between cilostazol peak and adjacent impurity peaks shall meet the requirements. 20 u1 of each of the above two solutions were accurately measured and injected into human liquid chromatography respectively, and the chromatogram was recorded to 2 times of the retention time of the main peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
- dissolution: according to the dissolution and release determination method (General rule 0931 second method), 0.3% sodium dodecyl sulfate solution is used as the dissolution medium, and the rotation speed is 75 rpm, after 30 minutes, take an appropriate amount of the solution, filter, take a precise amount of the filtrate, put it in a 25ml measuring flask, dilute it to the scale with the dissolution medium, shake it well, and use it as a test solution; another 20mg of cilostazol reference substance was added into a 100ml measuring flask, 15ml of methanol was added, dissolved by ultrasound, diluted to the scale with dissolution medium, and then shaken, in a 50ml measuring flask, dilute to the scale with the dissolution medium, shake well, and use the above two solutions as the reference solution. Take the above two solutions according to UV-Vis spectrophotometry (General rule 0401), the absorbance was measured at a wavelength of 257nm and the dissolution rate of each particle was calculated. The limit is 70% 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 difference of loading amount, grind them finely, mix them evenly, weigh the appropriate amount of fine powder (about equivalent to cilostazol lOmg ), put it in a 100ml measuring flask, and add the appropriate amount of methanol, sonicate cilostazol for 10 minutes, dilute to the scale with methanol, shake well, filter, Take 5ml of continuous filtrate precisely, put it in 50ml measuring flask, dilute to the scale with methanol, shake well, as a test solution; Another precision weigh the appropriate amount of cilostazol control, and methanol dissolved and quantitatively diluted to prepare a solution containing about 10ug per 1 ml, as a reference solution. The above two kinds of solutions were taken and the absorbance was measured at a wavelength of 257mn by ultraviolet-visible spectrophotometry (General rule 0401), and calculated.
category
Same as cilostazol.
specification
50mg
storage
sealed storage.
Last Update：2022-01-01 11:44:26
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Spot supply
Product Name: Cilostazol Visit Supplier Webpage Request for quotationCAS: 73963-72-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Cilostazol Visit Supplier Webpage Request for quotationCAS: 73963-72-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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