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Tacrolimus (Synonyms: Fujimycin; FR900506; FK506)

Cat. No.: HY-13756 Purity: 98.46%
Handling Instructions

Tacrolimus is a macrocyclic lactone with potent immunosuppressive properties. Tacrolimus binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase.

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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Other Forms of Tacrolimus:

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

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Tacrolimus is a macrocyclic lactone with potent immunosuppressive properties. Tacrolimus binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase.

    IC50 & Target

    PP2B (calcineurin phosphatase)[1]
    Autophagy inducer[2]

    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].

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 28 mg/mL (34.83 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.

      Tacrolimus (FK506) is prepared as an aqueous solution containing 6% cremophor EL and 6% ethanol[5]

    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 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.

    References
    Molecular Weight

    804.02

    Formula

    C₄₄H₆₉NO₁₂

    CAS No.

    104987-11-3

    SMILES

    O=C([[email protected]@](CCCC1)([H])N1C(C([[email protected]@]2(O)[[email protected]](C)C[[email protected]](OC)[[email protected]@](O2)([H])[[email protected]@H](OC)C[[email protected]@H](C)C/C(C)=C/[[email protected]]3CC=C)=O)=O)O[[email protected]](/C(C)=C/[[email protected]]4C[[email protected]@H](OC)[[email protected]](O)CC4)[[email protected]](C)[[email protected]@H](O)CC3=O

    Storage

    4°C, protect from light

    *The compound is unstable in solutions, freshly prepared is recommended.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.46%

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    Product Name:
    Tacrolimus
    Cat. No.:
    HY-13756
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    Tacrolimus

    Cat. No.: HY-13756