Molecular Weight: 804.018 (Some sources may mention 804.029, but the difference is minimal)
Physical Properties
Appearance: White or off-white crystalline powder
Density: 1.19 g/cm³
Melting Point: 113-115°C (Some sources may mention 186-190°C, which could be due to different measurement conditions)
Boiling Point: 871.7°C
Flash Point: 481.0°C
Solubility: Soluble in methanol, ethanol, acetone, ethyl acetate, chloroform, or ether. Difficult to dissolve in hexane or petroleum ether. Insoluble in water.
Chemical Properties
Tacrolimus binds to the cellular protein FKBP12, forming a high-affinity complex that inhibits the activity of calcineurin.
By inhibiting the release of interleukin-2 (IL-2), it comprehensively suppresses the function of T lymphocytes, which is 100 times stronger than cyclosporine (CsA).
Pharmacological Effects
As an immunosuppressant, Tacrolimus inhibits T-cell activation, proliferation, and differentiation, as well as the production and receptor expression of various lymphokines, thereby exerting an immunosuppressive effect.
It is used as a first-line drug in liver, kidney, and other organ transplants, effectively preventing and treating transplant rejection.
Additionally, Tacrolimus plays an active role in the treatment of autoimmune diseases such as atopic dermatitis (AD), systemic lupus erythematosus (SLE), and autoimmune eye diseases.
