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  1. Cell Cycle/DNA Damage Stem Cell/Wnt Cytoskeleton TGF-beta/Smad
  2. Organoid ROCK
  3. Y-27632 dihydrochloride

Y-27632 dihydrochloride 是一種具有口服活性的、ATP 競(jìng)爭(zhēng)性的 ROCK (Rho-kinase) 抑制劑 (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM)。Y-27632 dihydrochloride 表現(xiàn)出抗癲癇的作用。

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Y-27632 dihydrochloride Chemical Structure

Y-27632 dihydrochloride Chemical Structure

CAS No. : 129830-38-2

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10 mM * 1 mL in DMSO ¥770
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Customer Review

Other Forms of Y-27632 dihydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 312 篇科研文獻(xiàn)

WB
IF

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    Expression of CTC cluster-related (plakoglobin and CD44) and EMT-related (vimentin and E-cadherin, 4 days) proteins in LNCaP cells grown on different substrates after treatment with different inhibitors (Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl)).

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    Immunofluorescence imaging of LNCaP cells treated with the Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl). After the cells are cultured on different substrates for 3 days, inhibitors are added and incubated for 24 h.

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128.  [Abstract]

    MHCC-97H and Huh-7 cells co-transfected with control or supervillin-specific siRNA and a RhoA(WT), RhoA(V14), or RhoA(N19) plasmids for 48 h are treated with PBS or Y27632 2HCl (10 μM) for 16 h during hypoxia, and then assayed for phosphorylated p38 and ERK by immunoblotting. β-actin is used as the loading control

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 31;8(47):82506-82530.  [Abstract]

    SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) cells were either untreated (-) or treated (+) with 10mM Y27632 over a period of 48 hr. SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) clones were either untreated (-) or treated (+) with 10 mM Y27632 followed by stimulation without (-) or with (+) 5 ng/mL of TGFβ1 for 48 hr.

    查看 ROCK 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects[1][2][3][4].

    IC50 & Target[1]

    ROCK-I

    220 nM (Ki)

    ROCK-II

    300 nM (Ki)

    PKN

    3.1 μM (Ki)

    Citron kinase

    5.3 μM (Ki)

    PKCα

    73 μM (Ki)

    PKA

    25 μM (Ki)

    體外研究
    (In Vitro)

    Y-27632 dihydrochloride (1-5 μM;0-60 分鐘) 促進(jìn)脂肪組織來(lái)源的干細(xì)胞 (ADSCs) 的神經(jīng)元分化[3]。
    Y-27632 dihydrochloride (1-5 μM;0-60 分鐘) 誘導(dǎo) ADSCs 中 NSE、MAP-2 和巢蛋白的表達(dá)[3]。

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

    Western Blot Analysis[3]

    Cell Line: Adipose tissue-derived stem cells (ADSCs)
    Concentration: 20 μM
    Incubation Time: 24 hours
    Result: Resulted in the up-regulation of NSE, MAP-2 and nestin protein levels by 25.3, 3.1 and 2.5 fold, respectively, compared to control cells not treated by Y-27632.
    體內(nèi)研究
    (In Vivo)

    Y-27632 dihydrochloride (口服灌胃;30 mg/kg;每日一次;4 周) 預(yù)防二甲基亞硝胺誘導(dǎo)的大鼠肝纖維化[1]。
    Y-27632 dihydrochloride (口服灌胃;5- 10 mg/kg;once) 對(duì) PTZ 和 MES 誘發(fā)的癲癇有抗癲癇作用[2]

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

    Animal Model: Male Wistar rats injected with dimethylnitrosamine[1]
    Dosage: 30 mg/kg
    Administration: Oral gavage; 30 mg/kg; once daily; 4 weeks
    Result: Decreased the occurrence of dimethylnitrosamine-induced hepatic fibrosis and reduced the collagen and hydroxyproline content and α-smooth muscle actin expression in the liver.
    Animal Model: Male Swiss albino mice injected with PTZ (pentylenetetrazole) or induced by MES (maximal electroconvulsive shock)[2]
    Dosage: 5-10 mg/kg
    Administration: Oral gavage; 5-10 mg/kg; once
    Result: Prolonged the onset time of myoclonic jerks when compared with those observed in the saline group (P<0.05).
    Prolonged the onset time of clonic convulsions when compared with saline group (P<0.05).
    Prevented the occurrence of tonic hindlimb extensions and death.
    分子量

    320.26

    Formula

    C14H23Cl2N3O

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    H2O 中的溶解度 : 100 mg/mL (312.25 mM; 超聲助溶)

    DMSO 中的溶解度 : 50 mg/mL (156.12 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.1225 mL 15.6123 mL 31.2246 mL
    5 mM 0.6245 mL 3.1225 mL 6.2449 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.81 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.81 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。

    以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑: PBS

      Solubility: 220 mg/mL (686.94 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.98%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.1225 mL 15.6123 mL 31.2246 mL 78.0616 mL
    5 mM 0.6245 mL 3.1225 mL 6.2449 mL 15.6123 mL
    10 mM 0.3122 mL 1.5612 mL 3.1225 mL 7.8062 mL
    15 mM 0.2082 mL 1.0408 mL 2.0816 mL 5.2041 mL
    20 mM 0.1561 mL 0.7806 mL 1.5612 mL 3.9031 mL
    25 mM 0.1249 mL 0.6245 mL 1.2490 mL 3.1225 mL
    30 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6021 mL
    40 mM 0.0781 mL 0.3903 mL 0.7806 mL 1.9515 mL
    50 mM 0.0624 mL 0.3122 mL 0.6245 mL 1.5612 mL
    60 mM 0.0520 mL 0.2602 mL 0.5204 mL 1.3010 mL
    80 mM 0.0390 mL 0.1952 mL 0.3903 mL 0.9758 mL
    100 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7806 mL

    * 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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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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    產(chǎn)品名稱:
    Y-27632 dihydrochloride
    目錄號(hào):
    HY-10583
    需求量: