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Cat. No. Name Size Price Add Cart
KI0834Tacrolimus50 mg$144
Tacrolimus100 mg$272
Tacrolimus500 mg$688

Chemical Characteristic

Product NameTacrolimus
SynonymsFK 506, prograf, Advagraf, Protopic
CAS No.104987-11-3
Molecular Weight 804.02
FormulaC44H69NO12
Chemical Structure

Biological activities

Tacrolimus is a potent immunosuppressive drug. Tacrolimus is also a carbocyclic lactone-lactan isolated from Streptomycetes tsukubaensis. Tacrolimus is used as an immunosuppressant in transplantation medicine and immunological diseases. Tacrolimus ultimately blocks the T-cell response by inhibiting IL-2 transcription. Tacrolimus profoundly affects the maturation process of human epidermal Langerhans' cells.[1] Tacrolimus is also an inhibitor of IL-2 promoter activity with an IC50 of 0.012 nM. Tacrolimus inhibits CaN phosphatase in activated Jurkat cells with an IC50 of 0.18 nM.[2] In anti-CD3/CD2 system, tacrolimus inhibits Th1 cytokines (IL-2, IFN-γ), Th2 cytokines (IL-4, IL-5) and IL-3, GM-CSF (produced by both Th1 and Th2). Tacrolimus inhibits Th1 and Th2 cytokines with an IC50 ranging from 0.02 to 0.11 ng/mL. [3] Tacrolimus reduces the calcineurin (Cn) activity of T cells in vivo by the cumulative effects of several distinct mechanisms. [4] Tacrolimus can enhance experimentally induced irritant contact dermatitis and not to accelerate healing of irritant contact dermatitis and UVB erythema.[5]

Protocols

Tacrolimus is dissolved in ethanol at 1 or 0.5 mg/mL (alclometasone dipropionate) and further diluted in complete culture medium. [3]

References

[1] Panhans-Gross A, et al. Human epidermal Langerhans' cells are targets for the immunosuppressive macrolide tacrolimus (FK506). J Allergy Clin Immunol. 2001, 107(2): 345-352. 閵嗏偓閵嗏偓
[2] Peterson LB, et al. A tacrolimus-related immunosuppressant with biochemical properties distinct from those of tacrolimus. Transplantation. 1998, 65(1): 10-18. 閵嗏偓閵嗏偓
[3] Sakuma S, et al. Tacrolimus suppressed the production of cytokines involved in atopic dermatitis by direct stimulation of human PBMC system. (Comparison with steroids). Int Immunopharmacol. 2001, 1(6): 1219-1226. 閵嗏偓閵嗏偓
[4] Suzuki N, et al. In vivo mechanisms for the inhibition of T lymphocyte activation by long-term therapy with tacrolimus (FK-506): experience in patients with Beh?et's disease. Arthritis Rheum. 1997, 40(6): 1157-1167. 閵嗏偓閵嗏偓
[5] Fuchs M, et al. Tacrolimus enhances irritation in a 5-day human irritancy in vivo model. Contact Dermatitis. 2002, 46(5): 290-294. 閵嗏偓閵嗏偓

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