Fasudil dihydrochloride

SKU: orb1688655

Description

Fasudil dihydrochloride

Research Area

Cell Biology, Epigenetics & Chromatin, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 203911-27-7
• MW: 364.29
• Formula: C₁₄H₁₉Cl₂N₃O₂S
• SMILES: Cl.Cl.O=S(=O)(N1CCCNCC1)c1cccc2cnccc12
• Target: Others
• Solubility: H2O:≥ 80 mg/mL;DMSO:16 mg/mL (43.92 mM)

Bioactivity

• Target IC50:
  ROCK1 (p160ROCK):0.33 μM (Ki)|PKG:1.65 μM|PKA:4.58 μM|PKC:12.3 μM|ROCK2:0.158 μM
• In Vivo:
  Fasudil dihydrochloride (10 mg/kg, i.v., administered 1 hour before surgery) exhibits protective effects on the cardiovascular system under ischemic injury conditions, reduces the activation level of JNK, and attenuates the mitochondrial-nuclear translocation of AIF . Fasudil dihydrochloride (50 mg/kg/day, i.p.) can suppress acute and recurrent EAE induced by proteolipid protein PLP p139-151, inhibit lymphocyte proliferation, downregulate the expression of IL-17, and significantly reduce the IFN-γ/IL-4 ratio . Fasudil dihydrochloride (100 mg/kg/day, p.o.) significantly decreases the incidence and pathological scores of EAE in SJL/J mice, while alleviating inflammatory responses, demyelination, axonal loss in spinal cord tissues, and reducing the accumulation of APP-positive signals in the spinal cord .
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• In Vitro:
  Fasudil dihydrochloride (100 μM) can inhibit cell spreading, stress fiber formation, and α-SMA expression in rat hepatic stellate cells (HSCs) and human HSC-derived TWNT-4 cells, while also significantly suppressing the proliferation of these two cell types . Fasudil dihydrochloride (50–100 μM) can inhibit lysophosphatidic acid (LPA)-induced phosphorylation levels of ERK1/2, JNK, and p38 in rat hepatic stellate cells and human HSC-derived TWNT-4 cells . Fasudil dihydrochloride (25–100 μM, 24 h) can suppress the transcription of collagen and tissue inhibitor of metalloproteinases (TIMP), and simultaneously promote the transcription of matrix metalloproteinase-1 (MMP-1) in human HSC-derived TWNT-4 cells .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AT877 dihydrochloride, AT-877 dihydrochloride, HA1077 dihydrochloride, HA-1077 dihydrochloride

Compound Identifiers

PubChem CID

16219471