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Tacrolimus (FK506)
Catalog No.S5003 Synonyms: FR900506, Fujimycin, Prograf
For research use only.
Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.
CAS No. 104987-11-3
Selleck's Tacrolimus (FK506) has been cited by 65 publications
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Biological Activity
| Description | Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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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| 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 (from reference)
| References |
|---|
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 |
15mg/mL |
Chemical Information
| Molecular Weight | 804.02 | ||
|---|---|---|---|
| Formula | C44H69NO12 |
||
| CAS No. | 104987-11-3 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC | ||
In vivo Formulation Calculator (Clear solution)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05120570 | Not yet recruiting | Drug: VIC- 1911 | Acute Leukemia|Myelodysplastic Syndromes|Myeloproliferative Neoplasm|Lymphoma | Masonic Cancer Center University of Minnesota | February 2022 | Phase 1|Phase 2 |
| NCT05148715 | Not yet recruiting | Drug: Tacrolimus|Drug: Placebo | Organ Transplant Failure or Rejection|Brain Death|Ischemic Reperfusion Injury | Université de Sherbrooke|McMaster University | January 2022 | Phase 2 |
| NCT05005221 | Recruiting | Behavioral: Automated text messages | Kidney Transplant | University of Michigan | January 24 2022 | Not Applicable |
| NCT04505878 | Not yet recruiting | Drug: Vitamin C | Primary Graft Dysfunction|Lung Transplant; Complications | University of Wisconsin Madison | January 2022 | Phase 2 |
| NCT05152628 | Not yet recruiting | Drug: Tacrolimus granules | Liver Transplantation|Kidney Transplantation | Astellas Pharma China Inc.|Astellas Pharma Inc | December 31 2021 | Phase 4 |
| NCT05153915 | Not yet recruiting | Drug: Tacrolimus granules | Liver Transplantation|Kidney Transplantation | Astellas Pharma China Inc.|Astellas Pharma Inc | December 31 2021 | Phase 4 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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
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?
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).
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