Immunosuppressant that blocks T cell proliferation
in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 binding protein, thereby reversing its effects on sarcoplasmic reticulum Ca
2+ release. Inhibits the Ca
2+-dependent phosphatase, Protein Phosphatase 2B (Calcineurin; Cat. No.
539568), as well as Na
+,K
+-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of G
iα-3 protein.