Uses
immune suppressant, antifungal
Uses
FK-506 monohydrate has been used:
- as an immunosuppressive agent in coculture medium to study the effect of immunologic reaction
- as a calcineurin inhibitor, in anhydrous Me2SO solution
- to treat retinal pigment epithelial cells to measure possible cytotoxicity
Definition
ChEBI: A hydrate that is the monohydrate form of tacrolimus.
Biological Activity
Potent calcineurin (protein phosphatase 2B) inhibitor that requires FK 506-binding protein 12 (FKBP12) for activity (IC 50 = 3 nM). Inhibits secretion of IL-1, IL-2 (IC 50 = 1 nM), IL-3, IL-4, IL-6 (IC 50 = 35 nM), GM-CSF, TNF α (IC 50 = 10 nM), IFN γ and Myc from activated T-cells in vitro . Exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo .
Biochem/physiol Actions
FK-506 also appears to inhibit Na+/Ca2+ exchange. FK-506 and its derivatives demonstrate significant neurodegenerative activity. This property seems to arise via different mechanisms. FK-506 is also useful in treating ophthalmologic complications such as corneal graft rejection, uveoretinitis and allergen induced conjunctivitis.
Safety Profile
A poison by ingestion and intravenous routes. When heated to decomposition it emits toxic vapors of NOx.
