Tacrolimus

Tacrolimus

$96.00 - 25 mg

$336.00 - 100 mg

All prices in Australian dollars

Synonyms
Fujimycin, FK506, FR900506, Tskubaenolide
CAS #
104987-11-3
Molecular Formula
C44H69NO12
Molecular Weight
804
Purity
>95% by HPLC
Long Term Storage
-20°C
Solubility
Soluble in ethanol, methanol, DMF or DMSO. Limited water solubility.
Clear

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Application Notes

Tacrolimus (fujimycin) was discovered as a potent inhibitor of IL2 production in a targeted search for novel immunosuppressants. Tacrolimus acts by blocking T cell proliferation in vitro by inhibiting the generation of several lymphokines, notably the original target IL-2. Tacrolimus inhibits the activity of FK-506 binding protein, Ca2+-dependent phosphatase and calcineurin, and activates NF-κB through phosphorylation and degradation of IκBα.

References

  • FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. Kino T. et al., J. Antibiot. 1987, 40, 1249.
  • Cyclosporin A and FK506: molecular mechanisms of immunosuppression and probes for transplantation biology. Bierer B.E. et al., Curr. Opin. Immunol. 1993, 5, 763.
  • Immunosuppressant FK506 activates NF-kappaB through the proteasome-mediated degradation of IkappaBalpha. Requirement for Ikappabalpha n-terminal phosphorylation but not ubiquitination sites. Zhang Y. et al., J. Biol. Chem. 1999, 274, 34657.

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