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

Fasudil Hydrochloride  (Synonyms: 盐酸法舒地尔; HA-1077 Hydrochloride; AT-877 Hydrochloride)

目录号: HY-10341 纯度: 99.96%
COA 产品使用指南

Fasudil (HA-1077; AT877) Hydrochloride 是一种非特异性 RhoA/ROCK 抑制剂,并抑制蛋白激酶。Fasudil Hydrochloride 抑制 ROCK1Ki 为 0.33 μM,抑制 ROCK2PKAPKCPKGIC50 分别为 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil Hydrochloride 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Fasudil Hydrochloride Chemical Structure

Fasudil Hydrochloride Chemical Structure

CAS No. : 105628-07-7

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥565
In-stock
100 mg ¥513
In-stock
200 mg ¥705
In-stock
500 mg ¥1180
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Fasudil Hydrochloride:

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

    Fasudil Hydrochloride 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
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fasudil (HA-1077; AT877) Hydrochloride 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 Hydrochloride 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

    12.30 μM (IC50)

    PKG

    1.65 μM (IC50)

    体外研究
    (In Vitro)

    Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (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.

    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 24 hours
    Incubation Time: 24 hours
    Result: Reduced the expression of type I collagen, a-SMA, and TIMP-1.
    体内研究
    (In Vivo)

    Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (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

    327.83

    Formula

    C14H18ClN3O2S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    盐酸法舒地尔

    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, 1 years; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 55 mg/mL (167.77 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 31 mg/mL (94.56 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    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, 1 years; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.34 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.34 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 100 mg/mL (305.04 mM); 澄清溶液; 超声助溶

    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

    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
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.96%

    参考文献

    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, 1 years; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 / H2O 1 mM 3.0504 mL 15.2518 mL 30.5036 mL 76.2590 mL
    5 mM 0.6101 mL 3.0504 mL 6.1007 mL 15.2518 mL
    10 mM 0.3050 mL 1.5252 mL 3.0504 mL 7.6259 mL
    15 mM 0.2034 mL 1.0168 mL 2.0336 mL 5.0839 mL
    20 mM 0.1525 mL 0.7626 mL 1.5252 mL 3.8130 mL
    25 mM 0.1220 mL 0.6101 mL 1.2201 mL 3.0504 mL
    30 mM 0.1017 mL 0.5084 mL 1.0168 mL 2.5420 mL
    40 mM 0.0763 mL 0.3813 mL 0.7626 mL 1.9065 mL
    50 mM 0.0610 mL 0.3050 mL 0.6101 mL 1.5252 mL
    60 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2710 mL
    80 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.9532 mL
    H2O 100 mM 0.0305 mL 0.1525 mL 0.3050 mL 0.7626 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Fasudil Hydrochloride
    目录号:
    HY-10341
    需求量: