FK506 (Tacrolimus)

Catalog No.S5003 Batch:S500314

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Technical Data

Formula

C44H69NO12
Molecular Weight 804.02 CAS No. 104987-11-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (124.37 mM)
Ethanol 100 mg/mL (124.37 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tacrolimus (FK506) is a 23-membered macrolide lactone; it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein), creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Targets
FKBP12
(T cells)		 calcineurin
In vitro

Tacrolimus (FK506) and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. This compound prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. It binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). Tacrolimus specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. It and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. This compound binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs).

In Vivo

Tacrolimus (FK506) results in an increase in the paw and tail withdrawal threshold as revealed by behavioural pain assessment in rats against hyperalgesic and allodynic stimuli. It also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, a rise in tissue reduced glutathione levels in rats. This compound ameliorates the increase in neuronal oedema and axonal degeneration in rats with ischaemia reperfusion (I/R).

Protocol (from reference)

Cell Assay:

[3]
  • Cell Lines

    Jurkat cells

  • Concentrations

    10 nM

  • Incubation Time

    1 h

  • Method

    After cells were cultured with 10 nM Tacrolimus (FK506) for 1 hr and washed, phosphatase activity was measured in lysates.
Animal Study:

[8]
  • Animal Models

    Male C57BL/6J mice

  • Dosages

    30 mg/kg

  • Administration

    Oral

References

  • https://pubmed.ncbi.nlm.nih.gov/1715516/
  • https://pubmed.ncbi.nlm.nih.gov/1377361/
  • https://pubmed.ncbi.nlm.nih.gov/1373887/
  • https://pubmed.ncbi.nlm.nih.gov/7509138/
  • https://pubmed.ncbi.nlm.nih.gov/20529260/
  • https://pubmed.ncbi.nlm.nih.gov/18574318/
  • https://pubmed.ncbi.nlm.nih.gov/29863266/
  • https://pubmed.ncbi.nlm.nih.gov/22130237/

Customer Product Validation

<p>Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.</p>

Data from [ Biochim Biophys Acta , 2013 , 1833(3), 652-62 ]

<p>Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. I IL-17A, J TARC, K IL-13, L IL-1ra, M IL-5, N IL-10.</p>

, 2013 , Natural and Medical Sciences Institute

<p>Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. A IL-1β, B IL-6, C IFNγ, D MCP-1</p>

, 2013 , Natural and Medical Sciences Institute

<p>Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. E IL-8, F IP-10, G TNFα, H IL-4</p>

, 2013 , Natural and Medical Sciences Institute

Sellecks FK506 (Tacrolimus) Has Been Cited by 115 Publications

Calcineurin governs baseline and homeostatic regulations of non-rapid eye movement sleep in mice [ Proc Natl Acad Sci U S A, 2025, 122(4):e2418317122] PubMed: 39847332
Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa [ J Nanobiotechnology, 2025, 23(1):32] PubMed: 39844269
Calcium-mediated mitochondrial fission and mitophagy drive glycolysis to facilitate arterivirus proliferation [ PLoS Pathog, 2025, 21(1):e1012872] PubMed: 39804926
Interferon-gamma rescues dendritic cell calcineurin-dependent responses to Aspergillus fumigatus via Stat3 to Stat1 switching [ iScience, 2025, 28(2):111535] PubMed: 39898039
Signal transduction pathways controlling Ins2 gene activity and beta cell state transitions [ iScience, 2025, 28(3):112015] PubMed: 40144638
ACSL4 Drives C5a/C5aR1-Calcium-Induced Fibroblast-to-Myofibroblast Transition in a Bleomycin-Induced Mouse Model of Pulmonary Fibrosis [ Biomolecules, 2025, 15(8)1106] PubMed: 40867551
Polymeric-Based Theranostic Nanocarriers of Neuroprotective Drugs: Development, Imaging, and Bioanalysis [ Mol Pharm, 2025, 10.1021/acs.molpharmaceut.5c00170] PubMed: 40517330
Post-Liver Transplantation Management and Specimen Collection in Daurian Ground Squirrels for Single-Cell RNA Sequencing [ J Vis Exp, 2025, (223).] PubMed: 41052099
PU.1 and BCL11B sequentially cooperate with RUNX1 to anchor mSWI/SNF to poise the T cell effector landscape [ Nat Immunol, 2024, 25(5):860-872] PubMed: 38632339
Antiviral activity of immunosuppressors alone and in combination against human adenovirus and cytomegalovirus [ Int J Antimicrob Agents, 2024, 63(5):107116] PubMed: 38401774

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