2. Membrane Transporter/Ion Channel Neuronal Signaling Cytoskeleton Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Epigenetics Autophagy Anti-infection
  3. Calcium Channel ROCK PKA PKC Autophagy HIV
  4. Fasudil dihydrochloride

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

Cat. No.: HY-10341C Purity: 99.98%
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Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator.

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

Fasudil dihydrochloride

Fasudil dihydrochloride Chemical Structure

CAS No. : 203911-27-7

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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Fasudil dihydrochloride:

Fasudil dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    Fasudil dihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364.  [Abstract]

    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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    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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    ROCK ROCK1 ROCK2

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    PKA PKAR PKACα

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    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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    HIV HIV-1 HIV-2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].

    IC50 & Target

    PKA

    4.58 μM (IC50)

    PKC

    12.3 μM (IC50)

    PKG

    1.65 μM (IC50)

    p160ROCK

    0.33 μM (Ki)

    ROCK2

    0.158 μM (IC50)

    In Vitro

    Fasudil dihydrochloride (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4].
    Fasudil dihydrochloride (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4].
    Fasudil dihydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4].

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

    Fasudil dihydrochloride Related Antibodies

    Western Blot Analysis[4]

    Cell Line: Rat HSCs and human HSC-derived TWNT-4 cells
    Concentration: 50 μM; 100 μM
    Incubation Time: 24 hours
    Result: Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

    RT-PCR[4]

    Cell Line: Rat HSCs and human HSC-derived TWNT-4 cells
    Concentration: 25 μM; 50 μM; 100 μM
    Incubation Time: 24 hours
    Result: Reduced the expression of type I collagen, a-SMA, and TIMP-1.
    In Vivo

    Fasudil dihydrochloride (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[5].
    Fasudil dihydrochloride (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio[6].
    Fasudil dihydrochloride (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice[6].

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

    Animal Model: Myocardial ischemia and reperfusion in rat (250-300 g)[5]
    Dosage: 10 mg/kg
    Administration: Intravenous injection; 1 h before operation
    Result: Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
    Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.
    Clinical Trial
    Molecular Weight

    364.29

    Formula

    C14H19Cl2N3O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 100 mg/mL (274.51 mM)

    DMSO : 20.83 mg/mL (57.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7451 mL 13.7253 mL 27.4507 mL
    5 mM 0.5490 mL 2.7451 mL 5.4901 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.7451 mL 13.7253 mL 27.4507 mL 68.6266 mL
    5 mM 0.5490 mL 2.7451 mL 5.4901 mL 13.7253 mL
    10 mM 0.2745 mL 1.3725 mL 2.7451 mL 6.8627 mL
    15 mM 0.1830 mL 0.9150 mL 1.8300 mL 4.5751 mL
    20 mM 0.1373 mL 0.6863 mL 1.3725 mL 3.4313 mL
    25 mM 0.1098 mL 0.5490 mL 1.0980 mL 2.7451 mL
    30 mM 0.0915 mL 0.4575 mL 0.9150 mL 2.2876 mL
    40 mM 0.0686 mL 0.3431 mL 0.6863 mL 1.7157 mL
    50 mM 0.0549 mL 0.2745 mL 0.5490 mL 1.3725 mL
    H2O 60 mM 0.0458 mL 0.2288 mL 0.4575 mL 1.1438 mL
    80 mM 0.0343 mL 0.1716 mL 0.3431 mL 0.8578 mL
    100 mM 0.0275 mL 0.1373 mL 0.2745 mL 0.6863 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Fasudil dihydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Fasudil203911-27-7HA-1077AT-877HA1077HA 1077AT877AT 877Calcium ChannelROCKPKAPKCAutophagyHIVCa2+ channelsCa channelsRho-associated protein kinaseRho-associated kinaseRho-kinaseROKProtein kinase AProtein kinase CHuman immunodeficiency virusorally activeprotein kinasescollagena-SMATIMP-1ERK1/2JNKp38rat HSCshuman HSCTWNT-4 cellsCa2+ channel antagonistvasodilatorlysophoaphatidic acidLPAInhibitorinhibitorinhibit

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