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  3. Y-33075 dihydrochloride

Y-33075 dihydrochloride 

目录号: HY-10069 纯度: 98.75%
COA 产品使用指南

Y-33075 dihydrochloride是选择性的 ROCK 抑制剂,IC50 为 3.6 nM。

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Y-33075 dihydrochloride Chemical Structure

Y-33075 dihydrochloride Chemical Structure

CAS No. : 173897-44-4

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规格 价格 是否有货 数量
5 mg ¥729
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10 mg ¥1233
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25 mg ¥2870
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50 mg ¥4590
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100 mg ¥7340
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Other Forms of Y-33075 dihydrochloride:

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Top Publications Citing Use of Products

    Y-33075 dihydrochloride purchased from MCE. Usage Cited in: PLoS One. 2023 Jan 31;18(1):e0270288.  [Abstract]

    Y-27632 (10, 100 nM and 10, 100 µM; 24 h) decreases phosphorylation of MLC starting at a concentration of 100 nM in HSCs.

    Y-33075 dihydrochloride purchased from MCE. Usage Cited in: Neurotox Res. 2013 Apr;23(3):238-48.  [Abstract]

    Effect of Y39983 on glutamate-treated HT22 cell viability.

    查看 ROCK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.

    IC50 & Target

    ROCK

    3.6 nM (IC50)

    PKC

    420 nM (IC50)

    CaMKII

    810 nM (IC50)

    体外研究
    (In Vitro)

    Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively[1]. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983[2]. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution[3].

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

    体内研究
    (In Vivo)

    In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration[1]. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats[2].

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

    分子量

    353.25

    Formula

    C16H18Cl2N4O

    CAS 号
    性状

    固体

    颜色

    White to gray

    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
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (283.09 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)

    H2O 中的溶解度 : 50 mg/mL (141.54 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.8309 mL 14.1543 mL 28.3086 mL
    5 mM 0.5662 mL 2.8309 mL 5.6617 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。

    * 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: ≥ 2.5 mg/mL (7.08 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.08 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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 (283.09 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
    参考文献
    Kinase Assay
    [1]

    Recombinant ROCK (ROK α/ROCK II), purified protein kinase C (PKC: mixture of α, β, γ isoforms), and recombinant calmodulin-dependent protein kinase II (CaMK II) are used in the assay. ROCK (0.2 U/mL) is incubated with 1 μM [γ-32P] ATP and 10 μg/mL histone as substrates in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 20 minutes in 20 mM MOPS (3-(N-morpholino)propanesulfonic acid) buffer (pH 7.2) containing 0.1 mg/mL bovine serum albumin (BSA), 5 mM dithiothreitol [DTT], 10 mM β-glycerophosphate, 50 μM Na3VO4, and 10 mM MgCl2 in a total volume of 100 μL. PKC (10 ng/mL) is incubated with 1 μM [γ-32P] ATP and 20 μM PKC substrate in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 30 minutes in 20 mM MOPS buffer (pH 7.5) containing 0.1 mg/mL BSA, 10 mM DTT, 10 mM β-glycerophosphate, 50 μM Na3VO4, 2 mM CaCl2, 20 μg/mL phosphatidyl-l-serine, and 10 mM MgCl2 in a total volume of 100 μL. CaMK II (125 U/mL) is incubated with 1 μM [γ-32P] ATP, 10 μM calmodulin, and 20 μM CaMK II substrate, in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 30 minutes in 20 mM MOPS buffer (pH 7.5) containing 0.2 mg/mL BSA, 0.5 mM DTT, 0.1 mM β-glycerophosphate, 50 μM Na3VO4, 1 mM CaCl2, and 5 mM MgCl2 in a total volume of 100 μL. Incubation is terminated by the addition of 100 μL of 0.7% phosphoric acid. A 160 μL portion of the mixture is transferred to Multiscreen-PH plate. A positively charged phosphocellulose filter absorbs the substrate that binds 32P. The filter is washed with 300 μL of 0.5% phosphoric acid and then twice with purified water and then dried. The radioactivity of the dried filter is measured with a liquid scintillation counter. Results are presented as 50% inhibitory concentrations and 95% confidence intervals (CIs)[1].

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

    Cell Assay
    [2]

    In brief, retinal cell suspensions are obtained from dissected retinas of Wistar rats by papain treatment. Retinal ganglion cells (RGCs) are purified by the panning method using anti-rat CD11 antibody for removal of microglia cells and anti-rat Thy-1 antibody for isolation of ganglion cells. The purified RGCs (5000 cells/plate) are seeded into 24-well plates coated by 50 μg/mL of poly-l-lysine and 2 μg/mL of merosin, and are cultured in serum-free neurobasal medium supplemented with 2% B27 supplement, 50 ng/mL BDNF, 50 ng/mL CNTF, 5 μM forskolin, and 1 mM glutamine under a 95% air-5% CO2 atmosphere at 37°C. After completion of 24-hour cultivation, RGCs are cultured in medium with or without 10 μM Y-33075 as the final concentration for 24 hours and morphologically observed by phase-contrast microscopy. The concentration used is determined based on the effect of Y-33075 on trabecular meshwork contraction in vitro. Since this study is conducted in order to confirm whether Y-33075 has a potential of effect on axonal regeneration of RGCs, the effect is unquantitateively evaluated[2].

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

    Animal Administration
    [2]

    In brief, SD rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and the optic nerve of one eye is transected 4 to 6 mm posterior to the eyeball, taking care to avoid injury to the ophthalmic artery. The anterior branch of the sciatic nerve is excised and sutured autologously to the optic nerve stump with nylon sutures. The other end of the graft is sutured to the temporalis muscle. A small piece (3 mm × 3 mm) of gelatin sponge soaked with 10 μM Y-33075 or saline as a control is implanted in the space behind the optic stump after optic nerve transection in intact animals. Five μL of 0.12 mM or 1.2 mM Y-33075 solution or saline is administered into the vitreous body to final concentrations of 10 μM or 100 μM, respectively. The concentrations of Y-33075 used is determined as 10 μM that is effective in the in vitro study on axonal regeneration of RGCs, and also as 100 μM in order to confirm the dose response of Y-33075. Six weeks after surgery, rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and 4-Di-10ASP is embedded in the transplanted sciatic nerve to retrogradely label RGCs with axonal regeneration into the sciatic nerve. Three days after dye embedding, rats is euthanized and the eyes is enucleated for preparation of retinal flat-mounts. The posterior eyecup is then separated from the vitreous body and postfixed with 4% paraformaldehyde solution in phosphate buffer for around 1 hour at room temperature. Fluorescence micrographs of the labeled cells is imported using a fluorescence microscope connected to a computer. Labeled cells is counted using image analysis software. As a normal group, the subsequent procedure for retrograde labeling with 4-Di-10ASP is performed without grafting sciatic nerve and administering the test drug. Statistical analysis is performed using logarithmically transformed values due to differences in variance among the groups. The statistical significance of differences between the normal and saline groups and the saline and Y-33075 groups is examined by t-test (onesided) and William’s test (one-sided). Findings of p < 0.05 is considered significant[2].

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

    参考文献

    Y-33075 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
    H2O / DMSO 1 mM 2.8309 mL 14.1543 mL 28.3086 mL 70.7714 mL
    5 mM 0.5662 mL 2.8309 mL 5.6617 mL 14.1543 mL
    10 mM 0.2831 mL 1.4154 mL 2.8309 mL 7.0771 mL
    15 mM 0.1887 mL 0.9436 mL 1.8872 mL 4.7181 mL
    20 mM 0.1415 mL 0.7077 mL 1.4154 mL 3.5386 mL
    25 mM 0.1132 mL 0.5662 mL 1.1323 mL 2.8309 mL
    30 mM 0.0944 mL 0.4718 mL 0.9436 mL 2.3590 mL
    40 mM 0.0708 mL 0.3539 mL 0.7077 mL 1.7693 mL
    50 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4154 mL
    60 mM 0.0472 mL 0.2359 mL 0.4718 mL 1.1795 mL
    80 mM 0.0354 mL 0.1769 mL 0.3539 mL 0.8846 mL
    100 mM 0.0283 mL 0.1415 mL 0.2831 mL 0.7077 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。

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      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.

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    产品名称:
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    目录号:
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