2. Metabolic Enzyme/Protease
    Immunology/Inflammation
    Autophagy
    Apoptosis
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  3. Phosphatase
    FKBP
    Bacterial
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  4. Tacrolimus

Tacrolimus  (Synonyms: FK506; Fujimycin; FR900506)

Cat. No.: HY-13756 Purity: 99.93%
COA Handling Instructions

Tacrolimus (FK506), une lactone macrocyclique, se lie à la protéine de liaison FK506 (FKBP) pour former un complexe. Tacrolimus inhibe la calcineurine phosphatase, qui inhibe la transduction du signal des lymphocytes T et la transcription de l'IL-2. Les propriétés immunosuppressives.

Tacrolimus (FK506), ein makrozyklisches Lacton, bindet an das FK506 binding protein (FKBP) und bildet einen Komplex. Tacrolimus hemmt die calcineurin phosphatase, die die T-Lymphozyten-Signaltransduktion und die IL-2-Transkription hemmt. Immunsuppressive Eigenschaften.

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.

For research use only. We do not sell to patients.

Tacrolimus Chemical Structure

Tacrolimus Chemical Structure

CAS No. : 104987-11-3

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Customer Review

Based on 51 publication(s) in Google Scholar

Other Forms of Tacrolimus:

Top Publications Citing Use of Products

47 Publications Citing Use of MCE Tacrolimus

WB
IF

    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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    In Vitro

    Tacrolimus (FK506) 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.
    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
    Molecular Weight

    804.02

    Appearance

    Solid

    Formula

    C44H69NO12
    CAS No.
    SMILES
    Structure Classification
    Source

    fungus Streptomyces tsukubaensis.
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

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

    DMSO : ≥ 150 mg/mL (186.56 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1244 mL 0.6219 mL 1.2438 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 2.75 mg/mL (3.42 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (3.11 mM); Suspended solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.93%

    COA (322 KB) HNMR (348 KB) RP-HPLC (257 KB) MS (180 KB)

    Handling Instructions (2659 KB)
    References
    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.
    References
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    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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    Keywords:

    Tacrolimus104987-11-3FK506 Fujimycin FR900506FK 506FK-506FR900506FR 900506FR-900506PhosphataseFKBPBacterialAutophagyAntibioticFK506-binding proteinInhibitorinhibitorinhibit

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