1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
    Epigenetics
    Autophagy
  2. ROCK
    PKC
    Autophagy

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

Cat. No.: HY-10341 Purity: 99.92%
Data Sheet SDS Handling Instructions

Fasudil (Hydrochloride) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
200 mg $70 In-stock
500 mg $110 In-stock
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Other Forms of Fasudil Hydrochloride:

    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
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Fasudil (Hydrochloride) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

    IC50 & Target

    Ki: 0.33 μM (ROCK-II), 1.6 μM (PKA), 1.6 μM (PKG), 3.3 μM (PKC), 36 μM (MLCK)

    In Vitro

    Fasudil (Hydrochloride) has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit 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]. 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 suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK[5].

    In Vivo

    Fasudil (30 μg) produces an approximate 50% increase in CBF via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil 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 significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs[3]. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6]. The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice[7].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    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
    Molecular Weight

    327.83

    Formula

    C₁₄H₁₈ClN₃O₂S

    CAS No.

    105628-07-7

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.92%

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    Product Name:
    Fasudil Hydrochloride
    Cat. No.:
    HY-10341
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