Fasudil HCl

SKU: orb1304579

Description

Fasudil hydrochloride is a potent cell-permeable inhibitor of ROCK1, PKA, PKC, and MLCK with respective Ki values of 0.33 µM, 1.0 µM, 9.3 µM, and 55 µM. It is widely used in cardiovascular and neurological research to study Rho kinase signaling pathways in both cellular and animal models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 105628-07-7
• MW: 327.84
• Purity: >98%
• Formula: C₁₄H₁₇N₃O₂S · HCl
• SMILES: C1CNCCN(C1)S(=O)(=O)c1cccc2c1ccnc2.Cl
• Target: Kinase
• Solubility: Soluble in DMSO (up to 75 mg/ml) or in Water (up to 100 mg/ml).

Bioactivity

• Target IC50:
  ROCK2:0.158 μM|ROCK1:0.33 μM(Ki)|PKC:9.3 μM(Ki)|MLCK:55 μM(Ki)|PKG:1.65 μM|PKA:1.0 μM(Ki)
• In Vivo:
  Fasudil induces the disassembly of actomyosin fibers and inhibits cell migration, competitively suppressing Ca2+-induced depolarization and constriction of the rabbit aorta. It blocks contraction responses to KCl, serum phenylalanine, and prostaglandin F2α, and inhibits the proliferation of hepatic stellate cells, formation of stress fibers, and expression of α-SMA, while also repressing cell growth without inducing apoptosis. Fasudil curtails the phosphorylation of ERK1/2, JNK, and p38 MAPK induced by LPA. Additionally, it exerts vasodilatory effects by inhibiting the contraction induced by serotonin, noradrenaline, histamine, angiotensin, and dopamine.
• In Vitro:
  Intravenous injections of Fasudil at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg decreased mean blood pressure (MBP) and increased heart rate (HR), vertebral blood flow (VBF), cerebral blood flow (CBF), renal blood flow (RBF), and femoral blood flow (FBF) in a dose-dependent manner. A total Fasudil dose of 1.0 ng/mL enhanced cardiac output. Intracoronary injections of 30 μg Fasudil in experimental dogs resulted in approximately a 50% increase in CBF. Oral administration of Fasudil (dose of 100 mg/kg/day) significantly lowered the incidence and average maximum clinical score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice immunized with PLP p139-151. Fasudil inhibited the proliferation response of mouse spleen cells to antigens, demonstrating cardiovascular protective effects by reducing the activation of JNK and mitigating the mitochondrial translocation of apoptosis-inducing factor (AIF) in ischemic injury.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HA-1077

Compound Identifiers

PubChem CID

163751