103745-39-7
基本信息
盐酸法舒地尔
六氢-1-(5-异喹啉基磺酰基)-1H-1,4-二氮卓
FASUDIL
at877
hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine
HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE
HA 1077, DIHYDROCHLORIDE, 99+%
Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine
HA-1077：Eril
2,3,4,5,6,7-Hexahydro-1-(isoquinolin-5-ylsulfonyl)-1H-1,4-diazepine
5-(Hexahydro-1H-1,4-diazepine-1-ylsulfonyl)isoquinoline
物理化学性质
| 外观性状 | 盐酸法舒地尔(Fasudil Hydrochloride)：C14H17N3O2S?HCl。[105628-07-7]。从水结晶，熔点220.5℃。白色结晶性粉末，熔点219.3℃。水中溶解度在Ph=5.0～7.0时可达2×10-2mol/L。急性毒性LD50小鼠，大鼠(mg/kg)：67.5，59.9静脉注射；124.5，123.2皮下注射；273.9，335.0口服。 |
| 沸点 | 506.2±60.0 °C(Predicted) |
| 密度 | 1.289±0.06 g/cm3(Predicted) |
| 储存条件 | Store at RT |
| 溶解度 | H2O: >200 mg/mL |
| 酸度系数(pKa) | 9.73±0.20(Predicted) |
| 形态 | solid |
| 颜色 | white |
| 水溶解性 | Soluble in water or DMSO |
| CAS 数据库 | 103745-39-7(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319 |
| 防范说明 | P261-P305+P351+P338 |
| WGK Germany | 3 |
| RTECS号 | HM4031166 |
| 海关编码 | 29334900 |
| 毒性 | mouse,LD50,unreported,73500ug/kg (73.5mg/kg),United States Patent Document. Vol. #4678783, |
应用领域
制备方法
常见问题列表
|
p160ROCK 0.33 μM (Ki) |
ROCK2 0.158 μM (IC 50 ) |
PKA 4.58 μM (IC 50 ) |
PKC 12.3 μM (IC 50 ) |
PKG 1.65 μM (IC 50 ) |
Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil (50-100 μM; 24 hours) inhibits the LPA-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells.
Western Blot Analysis
| Cell Line: | Rat HSCs and human HSC-derived TWNT-4 cells |
| Concentration: | 50 μM; 100 μM |
| Incubation Time: | 24 hours |
| Result: | Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively. |
RT-PCR
| Cell Line: | Rat HSCs and human HSC-derived TWNT-4 cells |
| Concentration: | 25 μM; 50 μM; 100 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced the expression of type I collagen, a-SMA, and TIMP-1. |
Fasudil (intravenous injection; 0.01, 0.03, 0.1 and 0.3 mg/kg) 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. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (orally administration; 100 mg/kg/day) 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.