tacrolimus

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.

13-O-Desmethyl tacrolimus (13-DMT; 13-O-Demethyl FK 506) is the primary metabolite of Tacrolimus. It exhibits weaker immunosuppressive activity compared to Tacrolimus. This compound is primarily utilized in monitoring studies of Tacrolimus through the analysis of the 13-DMT/Tacrolimus ratio.

Tacrolimus anhydrous 8-epimer is a new l-pipecolic acid macrolide lactone, an important immunosuppressive drug that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2.

Tacrolimus-13C-D2 is the 13C and deuterated compound of Tacrolimus (TMSM-3393).

Tacrolimus (Standard) is a reference standard for research and analysis in studies involving Tacrolimus. Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Tacrolimus-[13C,D4] (Standard) is a reference standard of Tacrolimus-[13C,D4] intended for quantitative analysis, quality control, and related biochemical research applications.

Tacrolimus-BSA is a hapten-carrier protein conjugate formed by coupling Tacrolimus to bovine serum albumin (BSA). As a hapten, Tacrolimus alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Tacrolimus-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M TBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

Mycophenolic Acid Impurity (5,7-dihydroxy-4-methylphthalide) is an an immunosuppresant drug and potent anti-proliferative, and can be used in place of the older anti-proliferative azathioprine. It is usually used as part of triple therapy including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone. It is also useful in research for the selection of animal cells that express the E. coli gene coding for XGPRT (xanthine guanine phosphoribosyltransferase).

L 683519 is one of the Tacrolimus impurities with immunosuppressant and could restrain the activity of FK-506 binding protein.

L-732531 is a tacrolimus-related immunosuppressant with lower toxicity.

(E/Z)-FK-506 26,28-Allylic ester rearrangement impurity (FK506-A) is an impurity found in Tacrolimus.