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Fasudil

CAS No. : 103745-39-7

MCE 站：Fasudil

产品活性：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 K_i 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。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel  |  Autophagy  |  Protein Tyrosine Kinase/RTK  |  Epigenetics

作用靶点：ROCK  |  Calcium Channel  |  Autophagy  |  PKA  |  PKC

In Vitro: 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.

In Vivo: 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.

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