Free shipping on all orders over $ 500

Tacrolimus (FK506)

Cat. No. M1934
Tacrolimus (FK506) Structure
Synonym:

Fujimycin; FR900506; Prograf

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 36  USD40 In stock
50mg USD 58.5  USD65 In stock
100mg USD 108  USD120 In stock
200mg USD 162  USD180 In stock
1g USD 432  USD480 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

*The compound is unstable in solutions, freshly prepared is recommended

Product Citations
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).
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)."
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)."
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 804.02
Formula C44H69NO12
CAS Number 104987-11-3
Purity 99.73%
Solubility DMSO 90 mg/mL
Ethanol 80 mg/mL
Storage at -20°C
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.

Related Autophagy Products
Indophagolin

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively.

EN6

EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase).

Glycycoumarin

Glycycoumarin is a bioactive coumarin of licorice, it inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway.

TPEN

TPEN (TPEDA) is a specific cell-permeable heavy metal chelator.

Ginkgolide K

Ginkgolide K induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tacrolimus (FK506), Fujimycin; FR900506; Prograf supplier, Autophagy, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.