(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt
Enalapril Maleate
CAS: 76095-16-4
Molecular Formula: C24H32N2O9
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Names and Identifiers
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Physico-chemical Properties
| Molecular Formula | C24H32N2O9 |
| Molar Mass | 492.52 |
| Melting Point | 143-144,5°C |
| Boling Point | 0°C |
| Specific Rotation(α) | D25 -42.2° (c = 1 in methanol) |
| Flash Point | 0°C |
| Water Solubility | Soluble in water, methanol, and ethanol. |
| Solubility | Soluble in water (25 mg/ml), methanol (50 mg/ml), and ethanol (8 mg/ml). |
| Vapor Presure | 1.25E-24mmHg at 25°C |
| Appearance | White crystalline powder |
| Color | white to off-white |
| Maximum wavelength(λmax) | ['208nm(MeOH)(lit.)'] |
| Merck | 14,3567 |
| pKa | pKa1 3.0; pKa2 (25°) 5.4 |
| Storage Condition | 2-8°C |
| MDL | MFCD00133304 |
| Physical and Chemical Properties | White crystalline powder. The melting point was 140-147 °c. |
| Use | For renin-angiotensin antihypertensive drugs |
| In vitro study | Enalapril is rapidly converted by ester hydrolysis to enalaprilat, a potent ACE inhibitor; Enalapril itself is only a weak ACE inhibitor. Enalapril reduces peripheral vascular resistance without increasing heart rate. |
| In vivo study | In nnee mice, Enalapril blocks the deleterious effects of eNOS deficiency on blood pressure (BP), atherosclerosis, and renal insufficiency. In mdx mice, Enalapril caused a dose-dependent increase in forelimb strength. In the tibialis anterior muscle of mdx mice, Enalapril dose-dependently decreases superoxide anion production, as observed by dihydro-ethiene staining. Enalapril(5 mg/kg) reduced necrosis in both gastrocnemious muscle and septal muscle areas, while had no significant effect on non-muscle areas. In rats with bacterin (STZ)-induced diabetes (STZ-DM), Enalapril significantly increases kidney weight and urinary albumin concentration, as a result of Enalapril maleate, N-acetyl-FL-D-glucosamidase(NAG) and ET-1 in serum, and the concentration of ET-1 in the kidneys tends to increase. In the kidneys of diabetic rats, Enalapril caused increased mesangial cell proliferation, stromal expansion, and enlargement of the mesangial zone. In STZ-DM rats, Enalapril decreased increased urinary albumin and NAG concentrations, with slight improvement in electron microscopic changes. |
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Risk and Safety
| Risk Codes | R36/37/38 - Irritating to eyes, respiratory system and skin. R62 - Possible risk of impaired fertility R63 - Possible risk of harm to the unborn child |
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37 - Wear suitable protective clothing and gloves. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | 3077 |
| WGK Germany | 2 |
| RTECS | TW3666000 |
| HS Code | 29339900 |
| Toxicity | LD50 oral in rat: 2973mg/kg |
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Standard
Authoritative Data Verified Data
This product is N-[(S) -1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl-L-proline maleate. Calculated as dry product, containing C20H28N2O5 • C4H404 shall not be less than 98.5%.
Last Update：2024-01-02 23:10:35
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless, slightly hygroscopic.
- This product is soluble in methanol, slightly soluble in water, slightly soluble in ethanol or acetone, and almost insoluble in chloroform.
specific rotation
take this product, precision weighing, add methanol to dissolve and quantitative dilution to make a solution containing about 50mg per lml, according to the law (General 0621), the specific rotation is from -41.0°C to -43.5°C.
Last Update：2022-01-01 11:31:41
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Differential diagnosis
Authoritative Data Verified Data
- take about 20mg of this product, add 1ml of dilute sulfuric acid, drop add potassium permanganate solution, the red color will disappear.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 587).
Last Update：2022-01-01 11:31:42
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Exam
Authoritative Data Verified Data
acidity
take this product O.lg, add water 10ml to dissolve, according to the law (General 0631),pH value should be 2.0~2.8.
Related substances
take this product, add the mobile phase to dissolve and dilute to make a solution containing about 2mg per 1 ml, as a test solution; Take the appropriate amount of precision, quantitative dilution with mobile phase to prepare a solution containing about 20ug per lml as a control solution; Appropriate amount of maleic acid was taken, and the mobile phase was added to dissolve and dilute to prepare a solution containing about 0.5mg per lml; in addition, appropriate amounts of the enalaprilat (impurity I) control, the enalapril maleate control and the enalapril Dione (impurity II) control were separately taken, and the mobile phase was added to dissolve and dilute to prepare a mixed solution containing about 20ug each in 1 ml. According to the high performance liquid chromatography (General 0512) test, using octanosilane bonded silica gel as filler, phosphate buffer solution (0.Olmol / L potassium dihydrogen phosphate solution, adjusted to pH 2.2 with phosphoric acid)-acetonitrile (75:25) as mobile phase; The detection wavelength was 215nm; The column temperature was 50°C. Take 20 u1 of maleic acid solution and mixed solution, respectively inject human liquid chromatograph, record chromatogram, peak order: maleic acid peak, impurity I Peak, enalapril peak and impurity II peak, the tailing factor of enalapril peak should be less than 2.0, the separation degree between maleic acid peak and impurity I peak should meet the requirements, and the separation degree between impurity I Peak, enalapril peak and impurity II peak should be greater than 4.0. Accurately take 20 u1 of the test solution and the control solution respectively, inject them into the liquid chromatograph, record the chromatogram until the peak of impurity II is finished. If there is any impurity peak in the chromatogram of the test solution, the Peak area of individual impurities shall not be greater than 0.3 times (0.3%) The Peak area of enalapril in the control solution, and the sum of the peak areas of each impurity shall not be greater than the peak area of enalapril in the control solution (1.0%).
residual solvent
take about 0.3g of this product, weigh it accurately, place it in the top empty bottle, and add the internal standard solution accurately (weigh the appropriate amount of N-propanol, add N ,IV-dimethylformamide is made into a solution containing about 100ug per 1 ml) 3ml to dissolve, seal, as a test solution; In addition, ethanol, acetonitrile and dichloromethane in appropriate amounts are added for precision weighing, A mixed solution containing about 500ug of ethanol, 41ug of acetonitrile and 60ug of dichloromethane per 1 ml was prepared by quantitative dilution with an internal standard solution, and 3ml was accurately weighed, placed in a headspace bottle, sealed, and used as a reference solution. According to the test for determination of residual solvents (General rule 0861, second method), 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polar) was used as the stationary liquid; The initial temperature was 35 ° C. For 7 minutes, the temperature was increased to 200°C at a rate of 20°C per minute for 5 minutes; The inlet temperature was 220°C and the detector temperature was 220°C; The equilibrium temperature of the headspace bottle was 80°C, the equilibration time was 20 minutes. Take the reference solution into the headspace, the separation degree of each component peak should meet the requirements. Then the test solution and the reference solution were injected with headspace, and the chromatograms were recorded. According to the internal standard method to calculate the peak area, ethanol, acetonitrile and dichloromethane residues should be in accordance with the provisions.
loss on drying
take this product, at 60°C under reduced pressure drying to constant weight, weight loss should 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 retained residue shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 11:31:43
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Content determination
Authoritative Data Verified Data
take about 0.4g of this product, weigh it accurately, add 15ml of glacial acetic acid and anhydrous dioxane (take 500ml of dioxane, add 10g of dried 4A molecular sieve, place overnight, get 5ml), slightly temperature to dissolve, add crystal violet indicator liquid 1 drop, with perchloric acid titration solution (0.1 mol/L) titration to a clear blue color of the solution, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 49.25mg of C20H28N205. C4H404.
Last Update：2022-01-01 11:31:43
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Category
Authoritative Data Verified Data
angiotensin-converting enzyme inhibitors.
Last Update：2022-01-01 11:31:44
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:31:44
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Enalapril Maleate Tablets
Authoritative Data Verified Data
This product contains enalapril maleate (C20H28N2O5 • C4H4O4) should be 90.0% to 110.0% of label.
trait
This product is white or off-white.
identification
- take an appropriate amount of fine powder of this product (about 20mg of enalapril maleate), add 2ml of dilute sulfuric acid, stir, filter, add potassium permanganate solution to the filtrate, and the red color will disappear.
- 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
- relevant substances: take an appropriate amount of the fine powder of this product, add the mobile phase to dissolve and dilute to prepare a solution containing about 2mg of enalapril maleate per 1 ml as the test solution; Take an appropriate amount for precision measurement, A solution containing about 60ug per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.5 times (1.5%) of the peak area of enalapril in the control solution, the Peak area of impurity II shall not be greater than 1.0% of the peak area of enalapril in the control solution, and the peak area of other individual impurities shall not be greater than 0.5% of the peak area of enalapril in the control solution, the sum of each impurity peak area shall not be greater than the area of the enalapril peak in the control solution (3.0%).
- Content uniformity take 1 tablet of this product, put it in a measuring flask of 10ml( 2.5mg specification), 25ml(5mg specification) or 50ml( 10mg specification), add appropriate amount of water, shake to dissolve enalapril maleate, dilute with water to the scale, shake, filter, and determine the content according to the method under the content determination item, which shall comply with the regulations (General rule 0941).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), with water as the dissolution medium, the rotation speed is 100 rpm, after 30 minutes, take an appropriate amount of the solution, filter, and take the continued filtrate as the test solution; Take an appropriate amount of enalapril maleate reference substance, add water to dissolve and quantitatively dilute to make 5ug(2.5mg specification) per 1 ml, 10ug(5mg specification) or 20ug(10mg specification) solution, as a reference solution. The dissolution amount of each tablet was calculated as measured by the method under the content measurement item. The limit is 75% 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 octyl silane bonded silica gel as filler, phosphate buffer solution (0.01mol/L potassium dihydrogen phosphate solution, pH adjusted to 2.2 with phosphoric acid)-Acetonitrile (75:25) as mobile phase; Detection wavelength was 215mn; Column temperature was 50°C. Take an appropriate amount of maleic acid, add the mobile phase to dissolve and dilute to make a solution containing about 0.5mg of maleic acid per 1 ml; Take an appropriate amount of impurity I control, enalapril maleate control and impurity II control, respectively, the mobile phase was added to dissolve and dilute to prepare a mixed solution containing about 20ug each per 1 ml. 20 u1 of The maleic acid solution and the mixed solution were injected into the liquid chromatograph respectively, and the chromatograms were recorded. The order of peaks was maleic acid peak, impurity I Peak, enalapril peak and impurity II peak, the tailing factor of enalapril peak should be less than 2.0, the separation degree between maleic acid peak and impurity I peak should meet the requirements, and the separation degree between impurity I Peak, enalapril peak and impurity II peak should be greater than 4.0.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to 20mg enalapril maleate), 100ml flask, add appropriate amount of water, shake, dissolve enalapril maleate, dilute to the scale with water, shake well, filter, take the continued filtrate as a test solution, take a precise amount of 204, inject human liquid chromatography, record the chromatogram; an appropriate amount of reference substance of enalapril maleate was added with water for dissolution and quantitative dilution to prepare a solution containing about 0.2mg per 1 ml, which was determined by the same method and calculated by the peak area of enalapril according to the external standard method.
category
with enalapril maleate.
specification
- 2.5mg
- 5mg
- 10mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:31:45
(s)-1-(n-(1-(ethoxycarbonyl)-3-phenylpropyl)-l-alanyl)-l-proline (z)-2-butenedioate salt - Enalapril maleate capsules
Authoritative Data Verified Data
This product contains enalapril maleate (C20H28N2O5 • C4H404) should be 90.0% to 110.0% of the label.
trait
The content of this product is white or white particles or powder.
identification
- take an appropriate amount of the content of this product (about 20mg of enalapril maleate), add 2ml of dilute sulfuric acid, stir, filter, add potassium permanganate solution to the filtrate, and the red color will disappear.
- 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
- Related Substances: take an appropriate amount of fine powder of this product, dissolve it with mobile phase and dilute it to prepare a solution containing about 2mg of enalapril maleate per 1 ml as a test solution; Take an appropriate amount for precision measurement, A solution containing about 60ug per 1 ml was prepared by dilution with the mobile phase as a control solution. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.5 times (1.5%) of the peak area of enalapril in the control solution, the Peak area of impurity II shall not be greater than 1.0% of the peak area of enalapril in the control solution, and the peak area of other individual impurities shall not be greater than 0.5% of the peak area of enalapril in the control solution, the sum of each impurity peak area shall not be greater than the area of the enalapril peak in the control solution (3.0%).
- Content uniformity: Take 1 capsule of this product, pour the content into a 25ml ( 5mg specification) or 50ml ( 10mg specification) measuring flask, wash the capsule shell with water, wash the liquid and put it into the measuring flask, dilute with water to the scale, shake, filter, and determine the content according to the method under the content determination item, which shall comply with the regulations (General rule 0941).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 The first method), with water as the dissolution medium, the rotation speed is 100 rpm, after 30 minutes, take the appropriate amount of solution, filter, take the filtrate as the test solution; Take the appropriate amount of enalapril maleate reference substance, add water to dissolve and quantitatively dilute to make 10ug(5mg specification) per 1 ml. Or 20ug(10mg specification) of the solution, as a control solution. The dissolution amount of each pellet was calculated as measured by the method under the content measurement item. The limit is 75% 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
measured by high performance liquid chromatography (General 0512).
Chromatographic conditions and system applicability test with octanosilane bonded silica as filler, with phosphate buffer solution (0.Olmol / L potassium dihydrogen phosphate solution, adjusted to pH 2.2 with phosphoric acid)-acetonitrile (75:25) as mobile phase; The detection wavelength was 215nm; The column temperature was 50°C. Take appropriate amount of maleic acid, add mobile phase to dissolve and make a solution containing about 0.5mg of maleic acid per 1 ml; Take appropriate amount of impurity I reference, enalapril maleate reference and impurity II reference respectively, the mobile phase was added to dissolve and dilute to prepare a mixed solution containing about 20ug each per 1 ml. 20ul of The maleic acid solution and the mixed solution were injected into the liquid chromatograph, and the chromatograms were recorded. The order of peaks was maleic acid peak, impurity I Peak, enalapril peak and impurity II peak, the tailing factor of enalapril peak should be less than 2.0, the separation degree of maleic acid peak and enalaprilat peak should meet the requirements, and the separation degree between impurity I Peak, enalapril peak and impurity II peak should be greater than 4.0.
Determination of this product 20 capsules, precision weighing, calculate the average loading. Take the contents, mix well, grind finely, weigh an appropriate amount (about 20mg equivalent to enalapril maleate), put it in a 100ml measuring flask, add an appropriate amount of water, shake to dissolve enalapril maleate, dilute it with water to the scale, shake well, filter, take the filtrate as the test solution, take 20 u1 with precision, inject human liquid chromatograph, record the chromatogram; Take an appropriate amount of enalapril maleate reference substance, weigh it with precision, water was added to dissolve and quantitatively diluted to prepare a solution containing about 0.2mg per 1 ml, which was determined by the same method and calculated by the external standard method with the peak area of enalapril.
category
with enalapril maleate.
specification
(l)5mg (2)10mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:31:46
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Spot supply
Product Name: Enalapril Visit Supplier Webpage Request for quotationCAS: 76095-16-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Enalapril Maleate Request for quotation
CAS: 76095-16-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 76095-16-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Enalapril Maleate Visit Supplier Webpage Request for quotationCAS: 76095-16-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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