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Fasudil hydrochloride semihydrate

CAS No. : 186694-02-0

MCE 站：Fasudil hydrochloride semihydrate

产品活性：Fasudil (HA-1077; AT877) hydrochloride semihydrate 是一种非特异性 RhoA/ROCK 抑制剂，并抑制蛋白激酶。Fasudil hydrochloride semihydrate 抑制 ROCK1 的 K_i 为 0.33 μM，抑制 ROCK2，PKA，PKC，PKG 的 IC₅₀ 分别为 0.158 μM 和 4.58 μM，12.30 μM，1.650 μM。Fasudil hydrochloride semihydrate 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  |  Anti-infection  |  Epigenetics

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

In Vitro: Fasudil hydrochloride semihydrate (100 μM) inhibits cell spreading, the formation of stress fibers, ａnd expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) ａnd human HSC-derived TWNT-4 cells.
Fasudil hydrochloride semihydrate (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, ａnd p38 detected by western blotting in rat HSCs ａnd human HSC-derived TWNT-4 cells.
Fasudil hydrochloride semihydrate (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 hydrochloride semihydrate (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease ａnd reduces the activation of JNK ａnd attenuates mitochondrial-nuclear translocation of AIF under ischemic injury.
Fasudil hydrochloride semihydrate (50 mg/kg/d; i.p.) inhibits acute ａnd relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 ａnd a marked decrease of the IFN-γ/IL-4 ratio.
Fasudil hydrochloride semihydrate (100 mg/kg/d; p.o.) significantly reduces incidence ａnd pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss ａnd APP positivein spinal cord in mice.

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