Description General description An ethyl analog of FK506 with similar immunosuppressant properties. Acts by binding to immunophilins. Inhibits the synthesis of Th-1 and Th-2 type cytokines in target cells. Ethyl analog of FK-506 that possesses the same potent immunosuppressive properties as the parent compound. Inhibition of the Ca2+/calmodulin activated phosphatase calcineurin (IC50 = 10 nM) by the ascomycin/FK-506 binding protein complex is believed to be important in the mechanism of immunosuppression. Acts by binding immumophilins. Packaging 1 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: no Fully active via yeast rotamase (FK 506 binding protein) inhibition Primary Target Immunophilins Product does not compete with ATP. Reversible: no Warning Toxicity: Harmful (C) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Ethanol stock solutions are stable for up to 3 days at -20°C. Anhydrous DMSO stock solutions are stable for up to 1 month -20°C. Other Notes Paul, C., et al. 2000. Expert Opin. Invest. Drugs9, 69. Kawai, M., et al. 1993. FEBS Lett.316, 107. Pilot-Matias, T.J., et al. 1993. Gene128, 219. Shafiee, A., et al. 1993. J. Antibiot.46, 1397. Petros, A.M., et al. 1992. J. Med. Chem. 35, 2467.