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  2. 誘導疾病模型產(chǎn)品 Metabolic Enzyme/Protease Autophagy Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage Anti-infection
  3. 免疫與炎癥疾病模型 Phosphatase FKBP Bacterial Autophagy Antibiotic
  4. 半抗原
  5. Tacrolimus

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

目錄號: HY-13756 純度: 99.93%
COA 產(chǎn)品使用指南

Tacrolimus (FK506)，大環(huán)內(nèi)酯類，與 FK506 結(jié)合蛋白 (FKBP) 結(jié)合形成復合物并抑制鈣調(diào)神經(jīng)磷酸酶 (calcineurin phosphatase)，從而抑制 T 淋巴細胞信號轉(zhuǎn)導和 IL-2 轉(zhuǎn)錄。具有強免疫抑制特性。

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

Tacrolimus Chemical Structure

Tacrolimus Chemical Structure

CAS No. : 104987-11-3

1.  客戶無需承擔相應的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)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   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Tacrolimus:

MCE 顧客使用本產(chǎn)品發(fā)表的 78 篇科研文獻

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.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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

     

    細胞效力
    (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]
    體外研究
    (In Vitro)

    Tacrolimus (FK506) 抑制鈣依賴性事件，例如 IL-2 基因轉(zhuǎn)錄、NO 合酶激活、細胞脫顆粒和細胞凋亡。Tacrolimus 還通過與激素受體復合物中包含的 FKBPs 結(jié)合來增強糖皮質(zhì)激素和黃體酮的作用，防止降解。該試劑可以以類似于 CsA 的方式增強 TGFβ-1 基因的表達。Tacrolimus 抑制響應于 T 細胞受體連接的 T 細胞增殖[1]。低濃度 Tacrolimus (FK506，10 μg/L) 處理對 MH3924A 細胞增殖無顯著影響 (P=0.135)。用更高濃度的 Tacrolimus (100-1，000 μg/L) 處理后，MH3924A 細胞的增殖顯著增強 (P<0.01)。AMD3100 以任意濃度 (10、50、100 μg/L)，對 MH3924A 細胞增殖無明顯影響 (P>0.05)。然而，當不同濃度的AMD3100與100 μg/L Tacrolimus 聯(lián)用時，MH3924A 細胞的體外增殖能力增強 (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)

    通過從第 10 天到第 16 天或第 23 天對葡聚糖硫酸鈉 (DSS) 處理的小鼠施用 Tacrolimus 來研究 Tacrolimus 對結(jié)腸炎的進展和持續(xù)存在的處理效果。在第 17 天和第 24 天，結(jié)腸長度顯著縮短，結(jié)腸重量顯著縮短在 DSS 處理的對照動物中顯著高于正常動物。此外，對照組的單位長度結(jié)腸重量是正常組的兩倍多。雖然與對照組相比，用 Tacrolimus 處理 7 天和 14 天后顯著抑制了 DSS 處理動物每單位長度結(jié)腸重量的增加，但這種處理實際上并沒有恢復結(jié)腸縮短。此外，如抑制百分比 (59% 對 28%) 所示，Tacrolimus 對每單位長度結(jié)腸重量增加的抑制作用在 14 天時比在 7 天時更明顯[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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    他克莫司；藤霉素；他克莫斯；大環(huán)哌喃
    結(jié)構(gòu)分類
    初始來源

    fungus Streptomyces tsukubaensis.
    運輸條件

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

    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)
    細胞實驗： 

    DMSO 中的溶解度 : ≥ 150 mg/mL (186.56 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 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備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.75 mg/mL (3.42 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 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。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : 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)

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，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。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹慎選擇該方案。
    請確保第一步儲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: 99.93%

    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 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備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 1.2438 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.

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    Inquiry Information

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