FK506 (Tacrolimus)

CatalogusnummerS5003 Batch:S500315

Afdrukken

Technische gegevens

Formule

C44H69NO12
Moleculair gewicht 804.02 CAS-nr. 104987-11-3
Oplosbaarheid (25°C)* In vitro DMSO 100 mg/mL (124.37 mM)
Ethanol 100 mg/mL (124.37 mM)
Water Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 5.000mg/ml (6.22mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 2.500mg/ml (3.11mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving Tacrolimus (FK506) is een 23-ledige macrolide lacton; het vermindert peptidyl-prolyl isomerase activiteit in T-cellen door te binden aan het immunofiline FKBP12 (FK506 binding protein), waardoor een nieuw complex ontstaat. Tacrolimus remt ook de phosphatase activiteit van calcineurin. Tacrolimus induceert vasculaire endotheliale autophagy.
Doelen
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 behavioral 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, rise in tissue reduced glutathione levels in rats. This compound ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R).

Protocol (uit referentie)

Celassay:

[3]
  • Cellijnen

    Jurkat cells

  • Concentraties

    10 nM

  • Incubatietijd

    1 h

  • Methode

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

[8]
  • Dierlijke modellen

    Male C57BL/6J mice

  • Doseringen

    30 mg/kg

  • Toediening

    Oral

Referenties

  • 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/

Klantproductvalidatie

<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>

Gegevens van [ 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

Selleck's FK506 (Tacrolimus) Is geciteerd door 124 Publicaties

NFATc3 Enhances DREAM Complex-Driven Transactivation [ bioRxiv, 2026, 2026.01.12.699082] PubMed: 41648269
High-avidity TCR signaling induces a distinct KLR-positive exhaustion state in human tumor-infiltrating CD8 T cells associated with immunotherapy response [ bioRxiv, 2026, 2026.05.29.728765] PubMed: 42282651
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

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.