1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
    Neuronal Signaling
    Membrane Transporter/Ion Channel
    Autophagy
  2. ROCK
    Calcium Channel
    Autophagy
  3. Fasudil Hydrochloride

Fasudil Hydrochloride (Synonyms: HA-1077 (Hydrochloride); AT-877 (Hydrochloride))

Cat. No.: HY-10341 Purity: 99.91%
Handling Instructions

Fasudil Hydrochloride (HA-1077 Hydrochloride; AT-877 Hydrochloride), a potent inhibitor of ROCK with a Ki of 0.33 μM for ROCK1, which is also a potent Ca2+ channel antagonist and vasodilator.

For research use only. We do not sell to patients.

Fasudil Hydrochloride Chemical Structure

Fasudil Hydrochloride Chemical Structure

CAS No. : 105628-07-7

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Fasudil Hydrochloride:

Top Publications Citing Use of Products

    Fasudil Hydrochloride purchased from MCE. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364.

    RhoA and ROCK2 upregulation in the rat hippocampus is involved in memory dysfunction induced by postnatal exposure of Sevoflurane. The expression of RhoA, ROCK2 and cleaved caspase-3 (Cl-Csp3) in the hippocampus of the S3 group significantly increased, compared to that of the C group (P<0.05). There is no difference of the level of RhoA, ROCK2 and Cl-Csp3 between the C and S1 groups (P>0.05). ROCK2 inhibitor Fasudil hydrochloride in the F group clearly decreases the expression of ROCK2 and Cl-Cs

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    Description

    Fasudil Hydrochloride (HA-1077 Hydrochloride; AT-877 Hydrochloride), a potent inhibitor of ROCK with a Ki of 0.33 μM for ROCK1, which is also a potent Ca2+ channel antagonist and vasodilator.

    IC50 & Target[8]

    p160ROCK

    0.33 μM (Ki)

    In Vitro

    Fasudil Hydrochloride has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil inhibits contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a[2]. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction[3]. In addition, Fasudil induces disorganization of actin stress fiber and cell migration inhibition[4]. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil also blocks the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK[5].

    In Vivo

    Fasudil (30 μg) increases CBF by 50% via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) 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[3]. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6]. Fasudil (100 mg/kg/day, p.o.) 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[7].

    Clinical Trial
    Molecular Weight

    327.83

    Formula

    C₁₄H₁₈ClN₃O₂S

    CAS No.

    105628-07-7

    SMILES

    O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.Cl[H]

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 55 mg/mL (167.77 mM; Need ultrasonic)

    DMSO : ≥ 31 mg/mL (94.56 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0504 mL 15.2518 mL 30.5036 mL
    5 mM 0.6101 mL 3.0504 mL 6.1007 mL
    10 mM 0.3050 mL 1.5252 mL 3.0504 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Fasudil Hydrochloride
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