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

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

目录号: HY-10341C 纯度: 99.98%
COA 产品使用指南 技术支持

Fasudil (HA-1077; AT877) dihydrochloride 是一种非特异性 RhoA/ROCK 抑制剂，并抑制蛋白激酶。Fasudil dihydrochloride 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 dihydrochloride 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。

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Fasudil dihydrochloride

Fasudil dihydrochloride Chemical Structure

CAS No. : 203911-27-7

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25 mg ￥540
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50 mg ￥873
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100 mg ￥1350
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Customer Review

Other Forms of Fasudil dihydrochloride:

Fasudil dihydrochloride 相关抗体

Top Publications Citing Use of Products

    Fasudil dihydrochloride 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 Calcium Channel 亚型特异性产品:

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

    查看 ROCK 亚型特异性产品:

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    ROCK ROCK1 ROCK2

    查看 PKA 亚型特异性产品:

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    PKA PKAR PKACα

    查看 PKC 亚型特异性产品:

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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

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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)

    p160ROCK

    0.33 μM (Ki)

    ROCK2

    0.158 μM (IC50)

    PKG

    1.65 μM (IC50)

    体外研究
    (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].

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

    Fasudil dihydrochloride 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 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].

    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

    364.29

    Formula

    C14H19Cl2N3O2S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

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

    4°C, sealed storage, away from moisture

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

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 20.83 mg/mL (57.18 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献

    Fasudil dihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 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
    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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