FASUDEL
Fasudil hydrochloride
CAS: 105628-07-7
Molecular Formula: C14H18ClN3O2S
FASUDEL - Names and Identifiers
| Name | Fasudil hydrochloride |
| Synonyms | FASUDEL HA-1077 Fasudil HCL Fasudil hydrochloride HA-1077 DIHYDROCHLORIDE Fasudil Monohydrochloride (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE, 2HCL 1-(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE HYDROCHLORIDE 1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride HEXAHYDRO-1-(5-ISOQUINOLINYLSULFONYL)-MONOHYDROCHLORIDE 5-(1,4-DIAZEPAN-1-YLSULFONYL)ISOQUINOLINE HYDROCHLORIDE 1-(5-Isoquinolinesulfinyl)hexahydro-1H-1,4-diazepine hydrochloride Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine monohydrochloride |
| CAS | 105628-07-7 |
| EINECS | 805-833-0 |
| InChI | InChI=1/C14H17N3O2S.ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;/h1,3-5,7,11,15H,2,6,8-10H2;1H |
| InChIKey | LFVPBERIVUNMGV-UHFFFAOYSA-N |
FASUDEL - Physico-chemical Properties
| Molecular Formula | C14H18ClN3O2S |
| Molar Mass | 327.83 |
| Melting Point | 220.5°; mp 219.3° (Shirotani) |
| Boling Point | 506.2°C |
| Water Solubility | Soluble in water and dimethyl sulfoxide. Insoluble in ethanol. |
| Solubility | H2O: >200 mg/mL |
| Appearance | White solid |
| Color | white |
| Merck | 14,3942 |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month. |
| MDL | MFCD00943198 |
| Physical and Chemical Properties | Appearance white solid |
| Use | For the prevention and treatment of cardiovascular and cerebrovascular diseases |
| In vitro study | Fasudil is a class of calcium antagonists. Fasudil competitively inhibits Ca Fasudil also has vasodilatory effects, by inhibiting the contraction of helical strips induced by serotonin, norepinephrine, histamine, angiotensin, and dopamine. Fasudil induces the disintegration of actin fibers and inhibits cell migration. Fasudil inhibits the proliferation of hepatic stellate cells, the formation of stress fibers, and the expression of α-SMA, and inhibits cell growth, but does not induce apoptosis. Fasudil inhibits LPA-induced ERK1/2, JNK and p38 MAPK phosphorylation. |
| In vivo study | When Fasudil was administered at a dose of 30 μg by intracoronary injection to experimental dogs, the CBF increased by about 50%. Fasudil (0.01, 0.03, 0.1, and 0.3 mg/kg I. V.) decreased MBP and increased HR, VBF, CBF, RBF, and FBF in a dose-dependent manner. A total dose of 1.0 ng/mL of Fasudil increases cardiac output. Intravenous Fasudil treatment significantly reduced MBP, left ventricular systolic pressure, and total peripheral resistance, and increased HR and cardiac output, while right atrial pressure, there were no significant changes in dP/dt and work done by the left ventricle per minute. In the case of ischemic injury, Fasudil treatment has a protective effect on cardiovascular disease, and reduces the activation of JNK and inhibits mitochondrial AIF nuclear translocation. Daily oral administration of Fasudil at a dose of 100 mg/kg to SJL/J mice immunized with PLP p139-151 significantly reduced the incidence and the mean maximum value of EAE clinical score. Treatment of mice with Fasudil inhibits the proliferative response of splenocytes to antigen. Fasudil, administered orally to mice, reduces inflammation, and demyelination. |
FASUDEL - Risk and Safety
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | S36 - Wear suitable protective clothing. S60 - This material and its container must be disposed of as hazardous waste. |
| WGK Germany | 3 |
| RTECS | HM4031166 |
| HS Code | 29339900 |
| Toxicity | LD50 in mice, rats (mg/kg): 67.5, 59.9 i.v.; 124.5, 123.2 s.c.; 273.9, 335.0 orally (Koga) |
FASUDEL - Reference
| Reference Show more | 1. Hu Yanqiu, Hu Junhua, Sun Changhai, et al. Preparation of Fasudil Hydrochloride Liposome [J]. Heilongjiang Medical Science, 2017, v.40;No.224(06):28-30. |
FASUDEL - Standard
Authoritative Data Verified Data
This product is hexahydro-l-(5-isoquinolinesulfonyl)-l(H)-l, 4-diazepine hydrochloride, calculated as anhydrous, the content of C14H17N302S • HCl should be between 98.0% and 102.0%.
Last Update：2024-01-02 23:10:35
FASUDEL - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder. Odorless; Hygroscopic.
- This product is soluble in water, soluble in methanol, slightly soluble in ethanol, and almost insoluble in dichloromethane or ether.
Last Update：2022-01-01 15:06:49
FASUDEL - Differential diagnosis
Authoritative Data Verified Data
- take about 5mg of this product, put it in a small test tube, and use nickel hydroxide test paper at the test tube mouth [take the filter paper strip and immerse it in 30% nickel sulfate concentrated ammonia solution, take it out and dry it; after soaking in human lmol/ L sodium hydroxide solution for several minutes, the filter paper was covered with uniform nickel hydroxide precipitation, and the filter paper was taken out and washed with water (not to dry), and stored on wet cotton wool for later use], when heated, the green nickel hydroxide test paper shows black or gray spots.
- take this product, add water to dissolve and dilute to make a solution containing about 30ug per lml, according to UV-visible spectrophotometry (General 0401), at 275nm, there is maximum absorption at wavelengths of 312nm and 324nm, and minimum absorption at wavelengths of 250nm and 297nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1195).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:06:50
FASUDEL - Exam
Authoritative Data Verified Data
acidity
take 0.30g of this product, Add 10ml of water to dissolve it, and then measure it according to law (General rule 0631). The pH value should be 4.5-6.0.
clarity and color of solution
take 0.15g of this product, Add 10ml of water to dissolve, the solution should be clear and colorless; If it is turbid, compare with No. 1 turbidity standard solution (General rule 0902 first method) within 1 hour, should not be more turbid; If the color is developed, it should not be deeper compared with the yellow No. 1 Standard Colorimetric solution (General Principles 0901 first method).
Related substances
take this product, add mobile phase to dissolve and dilute to make a solution containing about 0.3mg per lml as a test solution; Take lml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. 5ml of the control solution was accurately measured, placed in a 100ml measuring flask, diluted to the scale with mobile phase, and shaken to serve as a sensitivity solution. According to the chromatographic conditions under the content determination item, take the sensitivity solution 20 u1, and inject the liquid chromatograph, so that the signal to noise ratio of the main component chromatographic peak should be not less than 10. 20 u1 of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded to 5 times of the retention time of the main component chromatographic peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.1 times (0.1%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%). The chromatographic peaks in the chromatogram of the test solution which are smaller than the main peak area of the sensitivity solution are ignored (0.05%).
residual solvent
N ,N-dimethylformamide take this product, precision weighing, plus internal standard solution (take the right amount of N-butanol, plus dimethyl sulfoxide to dissolve and dilute the right amount to make a solution containing 55ug per lml) dissolve and quantitatively dilute the solution containing 10 mg per 1 ml, as the test solution; Another precision weighing N ,N-dimethylformamide, A solution containing 88ug per 1 ml was prepared as a control solution by quantitative dilution with an internal standard solution. (0861) cyanopropylphenyl-(94%) dimethyl polysiloxane (or polar similar) as stationary liquid, according to the determination method of residual solvent (General Principles 100 third method), the temperature was maintained for 5 minutes and increased to 200°C at a rate of 20°C per minute, with an inlet temperature of 250°C and a detector temperature of 300°C. 1 u1 of the test solution and the reference solution are accurately measured, respectively injected into the human gas chromatograph, the chromatogram is recorded, and the peak area is calculated according to the internal standard method, which shall be in accordance with the regulations. The product is about 0.5g, precision weighed, placed in a 5ml measuring flask, and diluent [N,N-dimethylformamide-water (1:9)] is added. Dissolve and dilute to the scale, shake, as a test solution; Take ether 0.5g, methanol 0.3g and dichloromethane 0.06g, precision weighing, put in 100ml measuring flask, dilute to the scale with diluent, shake, take 1 ml in a 10ml measuring flask, dilute to the scale with diluent, shake well, and use as a reference solution. According to the determination method of residual solvent (General 0861 third method), the bonded/crosslinked polyethylene glycol (or similar polarity) is used as the stationary liquid, and the initial temperature is 45 C, and the solution is maintained for 2 minutes, the temperature was raised to 120°C at a rate of 40°C per minute for 5 minutes, the inlet temperature was 250°C, and the detector temperature was 250°C. 1 u1 of the test solution and the reference solution shall be accurately measured, respectively injected into the human gas chromatograph, the chromatogram shall be recorded, and the peak area shall be calculated according to the external standard method.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the water content shall not exceed 2.5%.
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 burning residues shall not contain more than 20 parts per million of heavy metals after examination by law (General rule 0821, Law II).
Last Update：2022-01-01 15:06:51
FASUDEL - 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; 1.0% triethylamine aqueous solution (adjusted to pH 7.0 with phosphoric acid)-methanol (50:50) was used as a mobile phase; The detection wavelength was 275nm. The number of theoretical plates shall not be less than 3000 calculated by fasudil, and the separation degree between fasudil peak and adjacent impurity peak shall meet the requirements.
assay
take about 15mg of this product, precision weighing, put it in 50ml measuring flask, add water to dissolve and dilute to the scale, shake, take 5ml precision, put it in 50ml measuring flask, dilute to scale with water, shake well, as a test solution, take 20u1 injection of human liquid chromatograph with precision, record chromatogram; Another precision weigh fasudil hydrochloride 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 15:06:52
FASUDEL - Category
Authoritative Data Verified Data
vasodilator.
Last Update：2022-01-01 15:06:52
FASUDEL - Category
Authoritative Data Verified Data
vasodilator.
Last Update：2022-01-01 15:06:52
FASUDEL - Storage
Authoritative Data Verified Data
sealed and stored in a dry place.
Last Update：2022-01-01 15:06:52
FASUDEL - Fasudil Hydrochloride Inj ection
Authoritative Data Verified Data
This product is a sterile aqueous solution of fasudil hydrochloride, containing fasudil hydrochloride (C14H17N302S • HCl) should be 90.0% ~ 110.0% of label.
trait
This product is colorless to yellowish clear liquid.
identification
- take the test solution under the content determination item, according to ultraviolet-visible spectrophotometry (General 0401), there is maximum absorption at 275nm, 312nm and 324nm wavelength, there is minimal absorption at wavelengths of 250Nm and 297nm.
- 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
- the pH value should be 4.0 to 6.3 (General 0631).
- the color of this product, compared with the yellow No. 1 Standard Colorimetric liquid (General Principles 0901 first method), should not be deeper.
- Related Substances: take this product and dilute it with mobile phase to make a solution containing 0.3mg per 1ml as a test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. 5ml of the control solution was accurately measured, placed in a 100ml measuring flask, diluted to the scale with mobile phase, and shaken to serve as a sensitivity solution. According to the method of fasudil hydrochloride related substances. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.2 times (0.2%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%). The chromatographic peaks in the chromatogram of the test solution which are smaller than the main peak area of the sensitivity solution are ignored (0.05%).
- bacterial endotoxin this product, according to the law inspection (General 1143), each 1 mg fasudil hydrochloride containing endotoxin amount should be less than 3.0EU.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
take 1ml of this product with precision, put it in 50ml measuring flask, dilute it with water to scale, shake it well, take 1ml with precision, put it in 10ml measuring flask, dilute it with water to scale, shake it well, as the test solution, it was obtained by the method under the item of fasudil hydrochloride content determination.
category
Same as fasudil hydrochloride.
specification
2ml:30mg
storage
light shielding, closed storage.
Last Update：2022-01-01 15:06:53
FASUDEL - Reference Information
| overview | fasudil hydrochloride is a new drug with extensive pharmacological effects. it was first developed by Asahi Kasei Company of Japan and first listed in Japan in June 1995. In 2001, China approved the import of fasudil hydrochloride injection by Asahi Kasei Company of Japan under the trade name of "Yililu". Its molecular structure is 5-isoquinoline sulfonamide derivative, which is an RHO kinase inhibitor. It expands blood vessels by increasing the activity of myosin light chain phosphatase, reduces the tension of endothelial cells, improves brain microcirculation, does not produce and aggravate brain steal blood, and can antagonize anti-inflammatory factors, protect nerves against apoptosis, and promote nerve regeneration. Fasudil hydrochloride has a certain effect on promoting the recovery of nerve function, reducing clinical symptoms and reducing disability rate. Therefore, due to the constraints of economic conditions and the degree of understanding of the disease at the grassroots level, ultra-early thrombolytic therapy cannot be achieved, but in order to reduce the further progress of the disease, it is very important to rebuild the local blood circulation within the treatment time window. Fasudil hydrochloride has significant neuroprotective and therapeutic effects on ischemic cerebrovascular diseases. It is worthy of clinical use, especially at the grassroots level, to reduce the disability rate and improve the quality of life. |
| Pharmacological effects | Fasudil hydrochloride is an isoquinoline sulfonamide derivative, which can not only inhibit the activity of free calcium ions in cells, but also inhibit protein kinase A.G.C and myoprotein light chain kinase, that is, inhibit smooth muscle contraction, the final stage of myosin light chain phosphorylation, make vascular smooth muscle relaxation, dilate blood vessels. In vitro experiments show that this product can relax the isolated cerebral blood vessels, inhibit the vasoconstriction caused by calcium ion influx, inhibit the contractile effect of various mechanisms of cerebrovascular constriction drugs, and inhibit intracellular calcium ions. The effect of vasoconstriction, but will not reduce the concentration of intracellular calcium ions, and inhibit the production of myosin light chain phosphorylates during vasoconstriction. It is clinically used to improve and prevent cerebral vasospasm and cerebral ischemia symptoms after subarachnoid hemorrhage. Intravenous administration of 30mg once, 2-3 times a day. This agent is applied in the early stage after subarachnoid hemorrhage, and it is generally appropriate to apply it for 2 weeks. When administered with 50~100mLNS or GS diluted intravenous drip, each intravenous drip time is 30 minutes. For patients with renal insufficiency, reduce the dose appropriately, for example, 10mg once. Adverse reactions after use may include intracranial hemorrhage, gastrointestinal hemorrhage, pulmonary hemorrhage, epistaxis, subcutaneous hemorrhage, disturbance of consciousness, etc. And liver dysfunction. Occasionally hypotension, anemia, leukopenia, renal dysfunction, polyuria, rash, fever, etc. Intracranial hemorrhage and possible intracranial hemorrhage patients, hypotension patients contraindicated. Preoperative diabetes, cerebral main artery arteriosclerosis, with severe disturbance of consciousness, subarachnoid hemorrhage with cerebrovascular disorders, liver and kidney dysfunction, patients over 70 years old, pregnant women and children with caution. Breast-feeding women should stop breastfeeding when taking medicine. This medicine can only be injected intravenously, and cannot be administered by other ways. |
| biological activity | Fasudil (HA-1077, AT-877) is an effective and selective Rho inhibitor (ROCK2, Ki = 0.33 μM), and also has inhibitory activity on PKA, PKG, PKC and MLCK, ki values are 1.6 μM, 1.6 μM, 3.3 μM and 36 μM respectively. Fasudil is also a blocker for calcium channel. |
| Target | Value |
| Rho () | |
| Calcium channel () | |
| ROCK2 (Cell-free assay) | 330 nM(Ki) |
| PKA (Cell-free assay) | 1.6 μM(Ki) |
| PKG (Cell-free assay) | 1.6 μM(Ki) |
| uses | cardiovascular and cerebrovascular drugs are used to improve the symptoms of ischemic cerebrovascular diseases caused by cerebral vasospasm after subarachnoid hemorrhage an effective Rho kinase inhibitor and vasodilator. At the same time, it also has inhibitory activity on PKA, PKG, PKC and MLCK. |
Last Update：2024-04-09 02:00:05
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