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

Fasudil  (Synonyms: 法舒地尔; HA-1077; AT877)

目录号: HY-10341A
产品使用指南

摩尔计算器

Fasudil (HA-1077; AT877) 是一种非特异性 RhoA/ROCK 抑制剂，并抑制蛋白激酶。Fasudil 抑制 ROCK1 的 Ki 为 0.33 μM，抑制 ROCK2，PKA，PKC，PKG 的 IC50 分别为 0.158 μM 和 4.58 μM，12.30 μM，1.650 μM。Fasudil 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 Fasudil Hydrochloride。

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Fasudil Chemical Structure

Fasudil Chemical Structure

CAS No. : 103745-39-7

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Fasudil 的其他形式现货产品:

Fasudil 相关抗体

Top Publications Citing Use of Products

    Fasudil purchased from MCE. 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

    查看 ROCK 亚型特异性产品:

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    ROCK ROCK1 ROCK2

    查看 Calcium Channel 亚型特异性产品:

    查看所有亚型
    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

    查看 PKA 亚型特异性产品:

    查看所有亚型
    PKA PKAR

    查看 PKC 亚型特异性产品:

    查看所有亚型
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fasudil (HA-1077; AT877) 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 is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].

    IC50 & Target[1]

    p160ROCK

    0.33 μM (Ki)

    ROCK2

    0.158 μM (IC50)

    PKA

    4.58 μM (IC50)

    PKC

    12.3 μM (IC50)

    PKG

    1.65 μM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HASMC IC50
    1.3 μM
    Compound: Fasudil
    Antiproliferative activity against human HASMC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
    Antiproliferative activity against human HASMC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
    		[PMID: 33569941]
    Sf9 IC50
    300 nM
    Compound: Fasudil
    Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
    Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
    		[PMID: 17018693]
    体外研究
    (In Vitro)

    Fasudil (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 (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 (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4].

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

    Fasudil 相关抗体:

    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.
    体内研究
    (In Vivo)

    Fasudil (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 (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 (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].

    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
    分子量

    291.37

    Formula

    C14H17N3O2S
    CAS 号
    中文名称

    法舒地尔
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Fasudil 相关分类

    • 摩尔计算器

    • 稀释计算器

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    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:

    Fasudil103745-39-7HA-1077 AT877法舒地尔HA1077HA 1077AT877AT 877AT-877ROCKCalcium ChannelAutophagyPKAPKCRho-associated protein kinaseRho-associated kinaseRho-kinaseROKCa2+ channelsCa channelsProtein kinase AProtein kinase Corally activeprotein kinasescollagena-SMATIMP-1ERK1/2JNKp38rat HSCshuman HSCTWNT-4 cellsCa2+ channel antagonistvasodilatorlysophoaphatidic acidLPAInhibitorinhibitorinhibit

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