Macrolide lactams
AdipoGen FK-506 Tacrolimus
Chemical. CAS 109581-93-3. Formula C44H69NO12 . H2O. MW 804.0 . 18.0. Isolated from Streptomyces FCZ0311. Potent immunosuppressant as cyclosporin A and rapamycin. Suppresses proliferation of cytotoxic T cells and inhibits the production of T cell-derived mediators such as interleukin-2 IL-2. Forms a complex with FK-506 binding protein 12 FKBP12. Inhibits the activity of the calcium/calmodulin-dependent protein phosphatase 2B PP2B calcineurin, leading to disruption of T cell activation. Prevents rejection of transplanted organs. Anti-inflammatory compound in the treatment of several inflammatory skin diseases e.g. atopic dermatitis and with potential anti-rheumatic activity rheumatoid arthritis. Neuroprotective. Regulates nitric oxide neurotoxicity. Neurotransmitter. Ca2 release compound. NF-kappaB suppressor by induction of unfolded protein response UPR. Anti-cancer compound. Apoptosis inducer.
Medchemexpress LLC Tacrolimus monohydrate | 109581-93-3 | 99.93% | 822.03 | 1 G
Tacrolimus monohydrate, a macrocyclic lactone, forms a complex by binding to FK506 binding protein (FKBP). This complex then inhibits calcineurin phosphatase, which in turn inhibits T-lymphocyte signal transduction and IL-2 transcription, leading to immunosuppressive properties. It also inhibits calcium-dependent events like IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus can potentiate the actions of glucocorticoids and progesterone by binding to FKBPs within the hormone receptor complex, preventing their degradation. The agent may also enhance the expression of the TGFβ-1 gene similarly to CsA, and it inhibits T cell proliferation in response to T cell receptor ligation.
- Enhances expression of the TGFβ-1 gene
- Inhibits T cell proliferation in response to T cell receptor ligation
- Immunosuppressive properties
- Inhibits calcineurin phosphatase