Tacrolimus (FK506)
Catalog No.S5003 Synonyms: FR900506
Molecular Weight(MW): 804.02
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.
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7 Customer Reviews
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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.
Biochim Biophys Acta 2013 1833(3), 652-62. Tacrolimus (FK506) purchased from Selleck.
FK506 reduces NCCE(Non-capacitative calcium entry) independently of its inhibitory effect in CaN activity. Fura-2-loaded human platelets were suspended in HBS medium containing 300 μM Ca2+ and preincubated for 5 min with increasing concentration of FK506 (0.5-50 μM), after which OAG (100 μM) was added to initiate NCCE.
Biochim Biophys Acta, 2015, 1853(10 Pt A):2684-96.. Tacrolimus (FK506) purchased from Selleck.
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FK506 production of S. tsukubaensis L19 and its recombinant pression of fkbN in S. tsukubaensis L19); L22, S. tsukubaensis L22 (overexpression of tcs7 in S. tsukubaensis L19); L23, S. tsukubaensis L23 (overexpression of fkbN and tcs7 in S. tsukubaensis L19).
J Ind Microbiol Biotechnol, 2016, 43(12):1693-1703.. Tacrolimus (FK506) purchased from Selleck.
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.
2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.
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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
2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.
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
2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.
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JCI Insight, 2016, 1(10):e86331.. Tacrolimus (FK506) purchased from Selleck.
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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. | ||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] FK-506 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. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4] |
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| Cell Data |
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| In vivo | FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 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. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 94 mg/mL (116.91 mM) |
|---|---|---|
| Ethanol | 83 mg/mL (103.23 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+corn oil For best results, use promptly after mixing. |
15mg/mL |
* 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.
Chemical Information
| Molecular Weight | 804.02 |
|---|---|
| Formula | C44H69NO12 |
| CAS No. | 104987-11-3 |
| Storage | powder |
| in solvent | |
| Synonyms | FR900506 |
Bio Calculators
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03603548 | Recruiting | Liver Transplant Rejection|Immunosuppression | Medical University of Warsaw | July 9 2018 | Not Applicable |
| NCT03194321 | Recruiting | End Stage Renal Disease | Cedars-Sinai Medical Center|Astellas Pharma Inc | May 9 2017 | Phase 4 |
| NCT02723591 | Recruiting | Kidney Transplantation | Astellas Pharma Global Development Inc.|Astellas Pharma Inc | September 9 2016 | Phase 4 |
| NCT01371331 | Completed | Kidney Transplantation|Heart Transplantation|Liver Transplantation | Astellas Pharma Europe Ltd.|Astellas Pharma Inc | June 9 2011 | Phase 4 |
| NCT03437577 | Enrolling by invitation | Kidney Transplant Failure and Rejection | University of Minnesota - Clinical and Translational Science Institute | May 8 2018 | Phase 1|Phase 2 |
| NCT03425071 | Recruiting | Kidney Transplantation|Rejection | University of Sao Paulo General Hospital|Maria da Luz Fernandes|Paschoalina Romano|Persio de Almeida Rezende Ebner|Nairo Massakazu Sumita|Veronica Porto Carreiro de Vasconcelos Coelho|Fabiana Agena|Elias David Neto|Nelson Zocoler Galante | March 8 2016 | -- |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions
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Question 1:
we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?
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Answer:
You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).
