2. 诱导疾病模型产品 Metabolic Enzyme/Protease Autophagy Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage Anti-infection
  3. 免疫与炎症疾病模型 Phosphatase FKBP Bacterial Autophagy Antibiotic
  4. 半抗原
  5. Tacrolimus

Tacrolimus  (Synonyms: 他克莫司; FK506; Fujimycin; FR900506)

目录号: HY-13756 纯度: 99.93%
COA 产品使用指南

摩尔计算器

Tacrolimus (FK506)，大环内酯类，与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶 (calcineurin phosphatase)，从而抑制 T 淋巴细胞信号转导和 IL-2 转录。具有强免疫抑制特性。

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

Tacrolimus Chemical Structure

Tacrolimus Chemical Structure

CAS No. : 104987-11-3

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
5 mg ￥312
In-stock
10 mg ￥500
In-stock
50 mg ￥700
In-stock
100 mg ￥1250
In-stock
200 mg ￥2000
In-stock
500 mg ￥3169
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Tacrolimus:

Tacrolimus 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 78 篇科研文献

IF
WB

    Tacrolimus 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 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 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 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 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 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 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.

    查看 Antibiotic 亚型特异性产品:

    查看所有亚型
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target

    Macrolide

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    B-cell IC50
    1.6 ng/mL
    Compound: FK-506
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    		[PMID: 14738397]
    CD4+ve Th IC50
    0.034 nM
    Compound: 1; FK506
    Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
    Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
    		[PMID: 33534559]
    Jurkat IC50
    0.056 nM
    Compound: 1, FK506
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    		10.1039/C2MD20266B
    Jurkat IC50
    0.19 nM
    Compound: FK-506
    Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
    Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
    		[PMID: 15369399]
    Jurkat IC50
    0.36 μM
    Compound: 1; FK-506
    Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA
    Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA
    		[PMID: 28412204]
    Jurkat IC50
    5.8 μM
    Compound: FK506
    Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA
    Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA
    		[PMID: 28509552]
    RBL-2H3 IC50
    0.25 nM
    Compound: FK506
    Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
    Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
    		[PMID: 23791076]
    RBL-2H3 IC50
    0.25 nM
    Compound: FK-506
    Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA
    Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA
    		[PMID: 22410084]
    T-cell IC50
    0.18 nM
    Compound: 1 (FK-506)
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    		10.1016/S0960-894X(01)81248-8
    T-cell IC50
    1.5 x 10-5 μg/mL
    Compound: FK-506
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    		[PMID: 14738397]
    U-251 IC50
    13.8 nM
    Compound: 1
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    		[PMID: 17643112]
    体外研究
    (In Vitro)

    Tacrolimus (FK506) 抑制钙依赖性事件，例如 IL-2 基因转录、NO 合酶激活、细胞脱颗粒和细胞凋亡。Tacrolimus 还通过与激素受体复合物中包含的 FKBPs 结合来增强糖皮质激素和黄体酮的作用，防止降解。该试剂可以以类似于 CsA 的方式增强 TGFβ-1 基因的表达。Tacrolimus 抑制响应于 T 细胞受体连接的 T 细胞增殖[1]。低浓度 Tacrolimus (FK506，10 μg/L) 处理对 MH3924A 细胞增殖无显著影响 (P=0.135)。用更高浓度的 Tacrolimus (100-1，000 μg/L) 处理后，MH3924A 细胞的增殖显著增强 (P<0.01)。AMD3100 以任意浓度 (10、50、100 μg/L)，对 MH3924A 细胞增殖无明显影响 (P>0.05)。然而，当不同浓度的AMD3100与100 μg/L Tacrolimus 联用时，MH3924A 细胞的体外增殖能力增强 (P<0.01)[3]。

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

    Tacrolimus 相关抗体:
    体内研究
    (In Vivo)

    通过从第 10 天到第 16 天或第 23 天对葡聚糖硫酸钠 (DSS) 处理的小鼠施用 Tacrolimus 来研究 Tacrolimus 对结肠炎的进展和持续存在的处理效果。在第 17 天和第 24 天，结肠长度显著缩短，结肠重量显著缩短在 DSS 处理的对照动物中显著高于正常动物。此外，对照组的单位长度结肠重量是正常组的两倍多。虽然与对照组相比，用 Tacrolimus 处理 7 天和 14 天后显著抑制了 DSS 处理动物每单位长度结肠重量的增加，但这种处理实际上并没有恢复结肠缩短。此外，如抑制百分比 (59% 对 28%) 所示，Tacrolimus 对每单位长度结肠重量增加的抑制作用在 14 天时比在 7 天时更明显[4]。

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

    804.02

    Formula

    C44H69NO12
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    他克莫司；藤霉素；他克莫斯；大环哌喃
    结构分类
    初始来源

    fungus Streptomyces tsukubaensis.
    运输条件

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

    4°C, protect from light

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

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 150 mg/mL (186.56 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 1.2438 mL 6.2188 mL 12.4375 mL
    5 mM 0.2488 mL 1.2438 mL 2.4875 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 (protect from light)。-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

    动物实验：

    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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.75 mg/mL (3.42 mM); 悬浊液; 超声助溶

    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (3.11 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。

      以 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。
    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

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

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.93%

    COA (300 KB) HNMR (214 KB) LCMS (142 KB) 元素分析报告 (221 KB)

    产品使用指南 (1538 KB)
    参考文献
    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 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.
    参考文献

    Tacrolimus 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 (protect from light)。-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 1.2438 mL 6.2188 mL 12.4375 mL 31.0938 mL
    5 mM 0.2488 mL 1.2438 mL 2.4875 mL 6.2188 mL
    10 mM 0.1244 mL 0.6219 mL 1.2438 mL 3.1094 mL
    15 mM 0.0829 mL 0.4146 mL 0.8292 mL 2.0729 mL
    20 mM 0.0622 mL 0.3109 mL 0.6219 mL 1.5547 mL
    25 mM 0.0498 mL 0.2488 mL 0.4975 mL 1.2438 mL
    30 mM 0.0415 mL 0.2073 mL 0.4146 mL 1.0365 mL
    40 mM 0.0311 mL 0.1555 mL 0.3109 mL 0.7773 mL
    50 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6219 mL
    60 mM 0.0207 mL 0.1036 mL 0.2073 mL 0.5182 mL
    80 mM 0.0155 mL 0.0777 mL 0.1555 mL 0.3887 mL
    100 mM 0.0124 mL 0.0622 mL 0.1244 mL 0.3109 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:

    Tacrolimus104987-11-3FK506 Fujimycin FR900506他克莫司藤霉素他克莫斯大环哌喃FK 506FK-506FR900506FR 900506FR-900506PhosphataseFKBPBacterialAutophagyAntibioticFK506-binding proteinInhibitorinhibitorinhibit

    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：
    Tacrolimus
    目录号：
    HY-13756
    需求量：

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * Lot #：

    * 客户姓名：

    		 

    * Email：

       电话：

    		 

    * 部门：

    * 公司或机构名称：

    		 

       留言给我们：

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    嗨！很高兴为您提供帮助！

    尊敬的 MCE 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z