法舒地尔

法舒地尔

中文名称法舒地尔
中文同义词法舒地尔;1-(5-硫代异喹啉)哌嗪二盐酸盐;六氢-1-(5-异喹啉基磺酰基)-1H-1,4-二氮卓;六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓;法舒地尔原料药;游离法舒地尔;HA 1077, DIHYDROCHLORIDE CALBIOCHEM
英文名称FASUDIL
英文同义词Fasudil Hydrochloride Injection;1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE;at877;hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine;HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE;HA 1077, DIHYDROCHLORIDE, 99+%;FASUDIL;Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine
CAS号103745-39-7
分子式C14H17N3O2S
分子量291.37
EINECS号816-154-4
相关类别抗心绞痛药;心脑血管药物;药物;小分子抑制剂;季铵盐类,相转移催化剂 Phase Transfer Catalysts;原料药;Protein Kinase Inhibitors and Activators;Protein Kinase;Signalling;Angiogenesis and Metastasis;Intracellular signaling;APIs;ERIL;对照品-杂质对照品;杂质对照品;医药原料药;原料药
Mol文件103745-39-7.mol
结构式法舒地尔 结构式

法舒地尔 性质

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
形态固体
酸度系数(pKa)9.73±0.20(Predicted)
颜色白色
水溶解性Soluble in water or DMSO
CAS 数据库103745-39-7(CAS DataBase Reference)

法舒地尔 用途与合成方法

研究人员表示,一种叫做法舒地尔的药物可以有效阻断反馈循环,保护阿尔茨海默氏症动物模型中的突触和记忆,同时减少大脑中β-淀粉样蛋白的含量。希望研究早日进入临床阶段,期待老年痴呆会在我们这一代人彻底绝迹。Fasudil (HA-1077; AT877) 是一种非特异性 RhoA/ROCK 抑制剂,对蛋白激酶也有抑制作用,ROCK1 的 Ki 值为 0.33 μM,ROCK2 和 PKA,PKC,PKG 的 IC50 值分别 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。

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.

化学性质 
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。
用途 
钙拮抗剂。用于蛛网膜下出血手术后的血管痉挛,也可用于神经保护、急性脑动脉栓塞、慢性脑梗死和心绞痛。
生产方法 
异喹啉经发烟硫酸磺化,生成的磺酸转化为磺酰氯,再和二氮革反应,得到产物。

安全信息

WGK Germany3
RTECS号HM4031166
海关编码29334900
毒性mouse,LD50,unreported,73500ug/kg (73.5mg/kg),United States Patent Document. Vol. #4678783,

MSDS信息

法舒地尔 上下游产品信息

上游原料
下游产品
"法舒地尔"相关产品信息
法舒地尔杂质 西尼必利 福沙吡坦二甲葡胺 CAL-101 西罗莫司脂化物 雷帕霉素 Ripasudil 埃克替尼 拉多替尼 奥拉西坦 尼莫地平 盐酸法舒地尔 盐酸法舒地尔 法舒地尔
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