Appearance：Clear slightly yellow liquid.
Stability：Stable at room temperature in closed containers under normal storage and handling conditions.
Vapor Pressure：2.22E-09mmHg at 25°C
27607-77-8, also known as FK-506, is a macrolide antibiotic derived from Streptomyces tsukubaensis which has been used as an immunosuppressant and antifungal agent since its development in 1983.
FK-506 is a 12-member macrolide lactone with a molecular weight of 822.98 g/mol. It exists in an amorphous, cream-colored powder form. It is soluble in water, chloroform, and benzene, and is slightly soluble in ethyl acetate, dimethyl sulfoxide, and toluene.
FK-506 binds to and inhibits the phosphatase calcineurin, thereby blocking the activation of nf-AT, a group of transcription factors that play an essential role in the induction of interleukin-2. Intracellularly, FK-506 binds to the cytosolic immunophilins, including FKBP-12, and inhibits calcineurin, blocking the activation of NF-AT. This inhibition leads to the suppression of lymphocyte induction of the proliferation and maturation of antigen-activated T-cells.
In addition to its use as an immunosuppressant, FK-506 also serves as an antifungal agent. The compound was found to inhibit the production of ergosterol, a fundamental component of fungal cell membranes and an important factor in fungal metabolism. By inhibiting the production of ergosterol, FK-506 is capable of inhibiting the growth and viability of fungal species.
FK-506 is currently used for the prevention of organ transplant rejection, the treatment of rheumatoid and psoriatic arthritis, Crohn's disease, and a variety of other autoimmune diseases, as well as for the treatment of fungal infections. The drug is also being investigated for use in the treatment of cancer and neurological disorders.