Tac Fk506 Pharmaceutical API 99% Tacrolimus Monohydrate Powder CAS 109581-93-3

CAS 109581-93-3 Pharmaceutical API Tac Fk506 9% Tacrolimus Monohydrate Powder

The Introductction of Tacrolimus

Tacrolimus, also known as FK506, is a macrolide isolated from Streptomyces spp. It has strong immunosuppressive effects, specifically binding to and inhibiting calmodulin phosphatase activity and inhibiting IL-2 signaling transcription, thereby inhibiting T-cell activation, TNF-α, IL-1β and IL-6 production, and T-cell-dependent B-cell proliferation. Compared with cyclosporine, another calmodulin phosphatase inhibitor, tacrolimus inhibits T-cell activation more strongly and has fewer adverse effects.
Clinical trials have shown that tacrolimus has good efficacy in heart, lung, intestinal, and bone marrow transplantation. Also FK506 plays an active role in the treatment of autoimmune diseases such as atopic dermatitis (AD), systemic lupus erythematosus (SLE), and autoimmune ophthalmopathy.
Tacrolimus is widely used for anti-rejection therapy after various organ transplants, as well as for the treatment of autoimmune diseases, renal diseases, and hematologic diseases. However, individual differences in tacrolimus administration are great, and a variety of drugs and foods may affect the blood concentration of tacrolimus at various stages of administration.
Tacrolimus monohydrate: C44H69NO12?H2O. colorless prismatic crystals from acetonitrile, melting point 127-129°C. [alpha]D20-84.4° (C=1.02, chloroform). Soluble in methanol, ethanol, aceton*, ethyl acetate, chloroform or ethyl ethe*, insoluble in hexane or petroleum ethe*, insoluble in water. Acute toxicity LD50 mice (mg/kg): >200 intraperitoneal injection. Acute toxicity LD50 male and female rats (mg/kg): 57.0, 23.6 intravenously; 134, 194 orally.

The Application & function of Tacrolimus

Tacrolimus is a macrolide antibiotic. Immunosuppressant. The mechanism of action is the same as cyclosporine, mainly inhibiting the synthesis of interleukin-2. It is used for rejection of organ transplantation and is more effective in acute rejection reactions.

Adverse effects
Tacrolimus can cause neurotoxicity, nephrotoxicity, glucose metabolism disorders and other adverse reactions, and is higher than cyclosporine. It can also cause infection, hypertension, hypercholesterolemia, hirsutism and other adverse reactions, but is lower than cyclosporine. Adverse reactions are related to the dose of the drug. Intravenous administration can cause hypertension, tremor, headache, insomnia, perceptual disorders, visual disabnormalities (e.g., cataracts, amblyopia), abnormal renal function (e.g., increased blood creatinine, increased or decreased urea nitrogen and urine output), constipation, diarrhea, nausea, hypercalcemia, hyperglycemia, hypophosphatemia, and leukocytosis. Occasionally there is leukopenia, anemia, allergic reactions, and increased potential for infection. Oral administration of this product is well tolerated, and adverse reactions are reduced accordingly.

Other Name of Tacrolimus

FK-506
TAC
TACROLIMUS
Tacrolimus monohydrate

The COA of Tacrolimus