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  2. Metabolic Enzyme/Protease Autophagy Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage Anti-infection
  3. Phosphatase FKBP Autophagy Bacterial Antibiotic
  4. Tacrolimus monohydrate

Tacrolimus monohydrate  (Synonyms: 他克莫司一水合物; FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate)

目錄號(hào): HY-13756A 純度: 99.67%
COA 產(chǎn)品使用指南

Tacrolimus monohydrate (FK506 monohydrate) 是大環(huán)內(nèi)酯類化合物，Tacrolimus monohydrate 與 FK506 結(jié)合蛋白 (FKBP) 結(jié)合形成復(fù)合物并抑制鈣調(diào)神經(jīng)磷酸酶 (calcineurin phosphatase)，從而抑制 T 淋巴細(xì)胞信號(hào)轉(zhuǎn)導(dǎo)和 IL-2 轉(zhuǎn)錄。具有強(qiáng)免疫抑制特性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Tacrolimus monohydrate Chemical Structure

Tacrolimus monohydrate Chemical Structure

CAS No. : 109581-93-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥588
In-stock
1 mg ￥225
In-stock
5 mg ￥450
In-stock
10 mg ￥650
In-stock
50 mg ￥990
In-stock
100 mg   詢價(jià)  
200 mg   詢價(jià)  

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Customer Review

Other Forms of Tacrolimus monohydrate:

MCE 顧客使用本產(chǎn)品發(fā)表的 78 篇科研文獻(xiàn)

IF
WB

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Cell Prolif. 2023 Mar 27;e13460.  [Abstract]

    FK506 (5 μM; 14?days) significantly inhibits the expression of WNT16b-promoting cell proliferation marker Ki67 and the putative hLESC marker ΔNp63α in hLESCs.

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Cell Prolif. 2023 Mar 27;e13460.  [Abstract]

    FK506 (5 μM; 14?days) inhibits WNT16b on hLESC cell proliferation.

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Cell Prolif. 2023 Mar 27;e13460.  [Abstract]

    FK506 (5 μM; 14?days) significantly inhibits the protein expression of both calcineurin A and NFATC2 in hLESCs.

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Cell Biol Toxicol. 2022 Jun;38(3):487-504.  [Abstract]

    FK506 inhibits dephosphorylation of Drp-1 at Ser637 site induced by CVB3 infection. CVB3 infection-induced decrease in Bcl-2 expression and enhanced levels of Bax and Caspase-3 cleavage are reversed by FK506.

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: J Extracell Vesicles. 2019 Dec 27;9(1):1709262.  [Abstract]

    Exosomal PD-L1 suppressed T cell activation and promoted skin cell migration in vitro (a). Representative confocal image show the appearance of exosomes as small-red dots. (b-c). Representative confocal images of pre-stained exosomes (red) colocalized with cell membrane (green) of HEK 293T (b) and Jurkat T cells (c).

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Brain Res. 2019 May 15;1711:68-76.  [Abstract]

    Levels of CytC in cytosol (Cyto-CytC), CytC in mitochondria (Mito- CytC) and cleaved caspase-3 in hippocampus are determined by western blot with the treatment of sham, HIR, MDV or FK506.

    Tacrolimus monohydrate purchased from MCE. Usage Cited in: Theranostics. 2018 Jan 1;8(4):878-893.  [Abstract]

    Accumulation of immune cells in host mice. Immunofluorescent images of CD4+ cells (green) in transplanted site in the normal, E+R, E+R+T, and E+R+T-RNPs groups at day 7 and day 21.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].

    IC50 & Target

    Macrolide

     

    體外研究
    (In Vitro)

    Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus[1]. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    The therapeutic effect of Tacrolimus is investigated on progression and perpetuation of colitis by administering Tacrolimus to Dextran sulfate sodium (DSS)-treated mice from Days 10 to 16 or to 23. At Days 17 and 24, colon length is significantly shortened, and colon weight is significantly higher in DSS-treated control animals than in normal animals. In addition, colon weight per unit length in the control group is more than twice that in the normal group. While both 7 and 14 d treatment with Tacrolimus significantly suppresses increases in colon weight per unit length in DSS-treated animals compared with the control group, this treatment does not actually restore the colon shortening. In addition, this inhibitory effect of Tacrolimus on increases in colon weight per unit length is more pronounced with 14-d than 7-d treatment, as shown by the inhibitory percentages (59% vs. 28%)[4].

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

    822.03

    Formula

    C44H71NO13
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    他克莫司一水合物；藤霉素一水合物
    結(jié)構(gòu)分類
    初始來源

    Streptomyces tsukubaensis
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

    DMSO 中的溶解度 : 100 mg/mL (121.65 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.2165 mL 6.0825 mL 12.1650 mL
    5 mM 0.2433 mL 1.2165 mL 2.4330 mL
    查看完整儲(chǔ)備液配制表

    * 請根據(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 (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.04 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。

      以 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

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.04 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，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      以 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玉米油中，混合均勻。

    動(dòng)物溶解方案計(jì)算器
    請輸入動(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

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.67%

    參考文獻(xiàn)
    Cell Assay
    [3]

    Tumor cell proliferation is determined by the MTT assay. Briefly, after MH3924A cells have reached the logarithmic growth phase, a 0.2-mL cell suspension at 1×104 cells/mL is added into each well of a 96-well plate and cultured in DMEM with 10% FBS, 10 μg/L vascular endothelial growth factor and 0.1 g/L heparin for 24 h. When adherent growth is established, different concentrations of Tacrolimus (10, 100 and 1,000 μg/L) , AMD3100 (10, 50 and 100 μg/L) and Tacrolimus (0 and 100 μg/L)+AMD3100 (0, 10, 50 and 100 μg/L) are added into the plates. Untreated cells cultured in medium alone are used as controls. After culturing for 48 h, 10 μL MTT (5 g/L) are added, and each well is incubated for 6 h; next, 150 μL/well DMSO are added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well is measured three times, and each sample is assayed in triplicate[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    Six-week-old male C57BL/6J mice are maintained in a temperature- and humidity-controlled room with a 12-h light-dark cycle. For the multiple dosing study, colitic mice (n=10) are orally administered Tacrolimus at 30 mg/kg for 7 d (Days 10 to 16) or 14 d (Days 10 to 23). Control (n=10) and normal groups (n=5) are administered placebo using the same regimen. Tacrolimus or placebo is administered at 10 mL/kg. Mice are euthanized by CO2 inhalation on the day following the final dosing. For the single dosing study, colitic mice are orally administered Tacrolimus at 30 mg/kg or placebo (n=8) once on Day 7, 10, 17, or 24. Normal mice (n=4) are administered placebo using the same regimen. Mice are euthanized by CO2 inhalation eight hours after dosing[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請根據(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 (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?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 1 mM 1.2165 mL 6.0825 mL 12.1650 mL 30.4125 mL
    5 mM 0.2433 mL 1.2165 mL 2.4330 mL 6.0825 mL
    10 mM 0.1217 mL 0.6083 mL 1.2165 mL 3.0413 mL
    15 mM 0.0811 mL 0.4055 mL 0.8110 mL 2.0275 mL
    20 mM 0.0608 mL 0.3041 mL 0.6083 mL 1.5206 mL
    25 mM 0.0487 mL 0.2433 mL 0.4866 mL 1.2165 mL
    30 mM 0.0406 mL 0.2028 mL 0.4055 mL 1.0138 mL
    40 mM 0.0304 mL 0.1521 mL 0.3041 mL 0.7603 mL
    50 mM 0.0243 mL 0.1217 mL 0.2433 mL 0.6083 mL
    60 mM 0.0203 mL 0.1014 mL 0.2028 mL 0.5069 mL
    80 mM 0.0152 mL 0.0760 mL 0.1521 mL 0.3802 mL
    100 mM 0.0122 mL 0.0608 mL 0.1217 mL 0.3041 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.

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    產(chǎn)品名稱：
    Tacrolimus monohydrate
    目錄號(hào)：
    HY-13756A
    需求量：