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

Tacrolimus monohydrate  (Synonyms: FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate)

Cat. No.: HY-13756A Purity: 99.67%
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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.

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

Tacrolimus monohydrate Chemical Structure

Tacrolimus monohydrate Chemical Structure

CAS No. : 109581-93-3

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10 mM * 1 mL in DMSO
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Based on 72 publication(s) in Google Scholar

Other Forms of Tacrolimus monohydrate:

Tacrolimus monohydrate Related Antibodies

Top Publications Citing Use of Products

65 Publications Citing Use of MCE Tacrolimus monohydrate

WB
IF

    Tacrolimus monohydrate purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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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    • References

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    Description

    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

     

    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].

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

    Tacrolimus monohydrate Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    822.03

    Formula

    C44H71NO13
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC=C)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O.O
    Structure Classification
    Initial Source

    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 : 100 mg/mL (121.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.67%

    COA (260 KB) HNMR (297 KB) RP-HPLC (100 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 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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
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    Tacrolimus monohydrate Related Classifications

    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:

    Tacrolimus109581-93-3FK506FujimycinFR900506FK 506FK-506FR 900506FR-900506PhosphataseFKBPAutophagyBacterialAntibioticFK506-binding proteinInhibitorinhibitorinhibit

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