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FK-506

Cat. No. M1934
FK-506 Structure
Synonym:

Tacrolimus, Fujimycin

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 110 In stock
50mg USD 80 In stock
200mg USD 210 In stock
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Quality Control
Biological Activity

FK-506 (also Tacrolimus or fujimycin) is a potent calcineurin (protein phosphatase 2B) inhibitor that requires FK 506-binding protein 12 (FKBP12) for activity (IC50 = 3 nM). FK-506 inhibits secretion of IL-1, IL-2 (IC50 = 1 nM), IL-3, IL-4, IL-6 (IC50 = 35 nM), GM-CSF, TNFα (IC50 = 10 nM), IFNγ and Myc from activated T-cells in vitro. FK-506 exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo. The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors. Furthermore, it has become clear that, predominantly as a result of CaN inhibition, FK506 alters multiple biochemical processes in a variety of cells besides lymphocytes. FK506 and ascomycin inhibit signaling pathways in astrocytes and change the pattern of cytokine and neurotrophin gene expression.

Protocol
Cell Experiment
Cell lines PMoH
Preparation method PMoH (2.5 x 105 cells/well) were seeded in 12-well plates and treated with various concentrations of the immunosuppressants. At 24, 48 and 72 hr post-treatment, wells were washed twice with sterile PBS and cells were fixed and stained with 0.1% crystal violet in 1M citric acid containing 20% methanol for 20 minutes at room temperature. Wells were washed thoroughly with sterile PBS to remove excess crystal violet and then air-dried. Bound dye was solubilized with 100 μl 100% DMSO for 20 minutes and the absorbance of the supernatants was measured at 544 nm using the FluoStar Optima (BMG LabTech) plate reader.
Concentrations 0.005 µg/ml
Incubation time 24, 48, 72 h
Animal Experiment
Animal models BDF1 mice
Formulation Solubilized in DMSO and diluted with PBS containing 10% dimethylacetamide (Sigma-Aldrich) and 6% Solutol (Sigma-Aldrich).
Dosages twice daily at 3.2, 10, 32 or 100 mg/kg for 5 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 804.02
Formula C44H69NO12
CAS Number 104987-11-3
Purity >99%
Solubility DMSO 150 mg/mL
Ethanol 150 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Univerrsite Pierre et Marie Curi (2015). Figure 4. FK-506 (Abmole Bioscience)
Method Electrophysiology
Cell Lines whole-cell
Concentrations 50 μM
Incubation Time 1 h
Results As shown in figure 4D, no plasticity could be induced in the 8 neurons challenged by the induction protocol in this condition (post-protocol IPSCs amplitude: 99 ± 11% of baseline, p>0.05).
Rating
Source The Journal of Neuroscience (2015). Figure 4.FK-506 from AbMole.
Method Electrophysiology patch-clamp technique
Cell Lines neuron
Concentrations incubated for 1 h in FK-506 (at 25 and 50 µM) and then perfused with 20 µM FK-506.
Incubation Time 1 h
Results "No plasticity could be induced in the eight neurons challenged by the induction protocol in this condition (postprotocol IPSC amplitude: 99 ± 4% of baseline, p>0.05)."
Rating
Source The Journal of Neuroscience (2015). Figure 4.FK-506 from AbMole.
Method Electrophysiology patch-clamp technique
Cell Lines neuron
Concentrations incubated for 1 h in FK-506 (at 25 and 50 µM) and then perfused with 20 µM FK-506.
Incubation Time 1 h
Results "No plasticity could be induced in the eight neurons challenged by the induction protocol in this condition (postprotocol IPSC amplitude: 99 ± 4% of baseline, p>0.05)."
Rating
Product Citations
References

Ascomycin and FK506: pharmacology and therapeutic potential as anticonvulsants and neuroprotectants.
Sierra-Paredes G, et al. CNS Neurosci Ther. 2008 Spring;14(1):36-46. PMID: 18482098.

Pharmacokinetic animal PET study of FK506 as a potent neuroprotective agent.
Murakami Y, et al. J Nucl Med. 2004 Nov;45(11):1946-9. PMID: 15534067.

FK506, an immunosuppressant targeting calcineurin function.
Dumont FJ. Curr Med Chem. 2000 Jul;7(7):731-48. PMID: 10702636.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: FK-506, Tacrolimus, Fujimycin supplier, inhibitors

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