概述 生物活性 靶点 体外研究 体内研究
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法舒地尔

法舒地尔,103745-39-7,结构式
法舒地尔
  • CAS号:103745-39-7
  • 英文名:FASUDIL
  • 中文名:法舒地尔
  • CBNumber:CB3101698
  • 分子式:C14H17N3O2S
  • 分子量:291.37
  • MOL File:103745-39-7.mol
法舒地尔化学性质
  • 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 :solid
  • 酸度系数(pKa) :9.73±0.20(Predicted)
  • 颜色 :white
  • 水溶解性 :Soluble in water or DMSO
  • CAS 数据库 :103745-39-7(CAS DataBase Reference)
安全信息
  • 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,

法舒地尔性质、用途与生产工艺

  • 概述 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。
  • 生物活性 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。
  • 靶点

    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 )

  • 体外研究

    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.
  • 体内研究

    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。
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