- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: Fasudil Hydrochloride
- Price:
- Purity: 99.0%
- Stocking Period: 10 Day
- Contact: Huang
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: Fasudil Hydrochloride
- Price: ￥1818.0/100mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Fasudil-HA
- Price: $350.0/1g $150.0/10ml
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- ShangHai DC Chemicals Co.,Ltd
- China
- Product Name: Fasudil-HA
- Price: ￥Inquiry/1g
- Purity: 98.9%
- Stocking Period: 1 Day
- Contact: Tony Lai
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: Fasudil hydrochloride
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
105628-07-7
105628-07-7 structure
- Name: Fasudil Hydrochloride
- Chemical Name: Fasudil Hydrochloride
- CAS Number: 105628-07-7
- Molecular Formula: C14H18ClN3O2S
- Molecular Weight: 327.83
- Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
- Create Date: 2018-08-25 09:47:18
- Modify Date: 2024-01-02 16:30:24
-
Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
| Name | Fasudil Hydrochloride |
|---|---|
| Synonyms |
5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline hydrochloride (1:1)
Eril 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride MFCD00943198 Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride (1:1) Fasudil HCl Fasudil Monohydrochloride 1-(5-Isoquinolinesulfonyl)homopiperazine Hydrochloride Fasudil Hydrochloride 5-(1-Homopiperazinyl)sulfonylisoquinoline Hydrochloride Fasudil (Hydrochloride) |
| Description | Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. |
|---|---|
| Related Catalog | |
| Target |
p160ROCK:0.33 μM (Ki) PKA:1 μM (Ki) PKC:9.3 μM (Ki) MLCK:55 μM (Ki) |
| In Vitro | Fasudil Hydrochloride has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil inhibits contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a[2]. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction[3]. In addition, Fasudil induces disorganization of actin stress fiber and cell migration inhibition[4]. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil also blocks the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK[5]. |
| In Vivo | Fasudil (30 μg) increases CBF by 50% via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs[3]. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6]. Fasudil (100 mg/kg/day, p.o.) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration[7]. |
| Kinase Assay | Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter. |
| References |
| Boiling Point | 506.2ºC at 760 mmHg |
|---|---|
| Melting Point | 222 °C(dec.) |
| Molecular Formula | C14H18ClN3O2S |
| Molecular Weight | 327.83 |
| Flash Point | 259.9ºC |
| PSA | 70.68000 |
| LogP | 4.17030 |
| Water Solubility | H2O: >200 mg/mL |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
| Hazard Codes | Xi |
|---|---|
| WGK Germany | 3 |
| RTECS | HM4031166 |
| HS Code | 2942000000 |
|
~%
105628-07-7 |
| Literature: EP1726306 A1, ; Page/Page column 5 ; |
|
~%
105628-07-7 |
| Literature: Chemical and Pharmaceutical Bulletin, , vol. 40, # 3 p. 770 - 773 |
| Precursor 3 | |
|---|---|
| DownStream 0 | |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |