Fasudil hydrochloride

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

Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 105628-07-7
• MW: 327.83
• Purity: >99.99% (May vary between batches)
• Formula: C₁₄H₁₈ClN₃O₂S
• SMILES: C1CNCCN(C1)S(=O)(=O)c1cccc2c1ccnc2.Cl
• Target: Serine/threonin kinase,ROCK,Calcium Channel,PKC,HIV Protease,Autophagy,PKA
• Solubility: H2O:32.8 mg/mL (100.05 mM);DMSO:82 mg/mL (250.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (10.07 mM)

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: keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CalciumChannel, collagen, Calcium Channel, Ca2+ channel antagonist, a-SMA, AT 877, AT877, AT-877, AT-877 hydrochloride, Autophagy, lysophoaphatidic acid, LPA, MLCK, Fasudil, Fasudil (HA-1077) HCl, Fasudil HCl, ERK1/2, HA 1077, HA 1077 Hydrochloride, HA1077, HA1077 Hydrochloride, HA-1077 hydrochloride, human HSC, HIVProtease, HIV Protease, HIV, Protein kinase A, protein kinases, ROCK, ROCK2, rat HSCs, TIMP-1, PKA, PKG, PKC, p38, Serine kinase, threoninkinase, Serinekinase, threonin kinase, TWNT-4 cells

Compound Identifiers

PubChem CID

163751