BOC Sciences Tacrolimus Analogue Set Product
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from the Health category at
06 Jul 2023 07:44:37 am.
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BOC Sciences have been committed to providing customers with high-quality tacrolimus and its analogues at the best price. These metabolites are fermentated and separated from microorganisms.
Our Tacrolimus Analogue Set includes:
Tacrolimus (FK-506)
Ascomycin
Tacrolimus impurities
We provide fermentation CDMO services from lab scale to GMP production. We have the ability to provide customized tacrolimus analogues for customers in the pharmaceutical and other industries.
About Tacrolimus
Tacrolimus (FK-506) is a novel macrolide antibiotic with high immunosuppressive effect. It was first isolated from Streptomyces tsukuba in 1984, and its capsule and injection preparations were officially marketed in 1993.
The chemical structure of Tacrolimus is unique, including the piperidine unit of the skeleton ring, the 4-hydroxy-3-methoxy cyclohexyl functional group, and the methoxy and allyl side chains. Tacrolimus, Ascomycin and Rapamyciny share many similarities in chemical structure, which are natural structural analogues. All three polyketone rings contain the same piperidine unit, and a side chain containing 4-hydroxy-3-methoxy cyclohexyl structure. However, Tacrolimus is more similar to Ascomycin that containing two methoxy side chains at the same location. The only difference between the two is that tacrolimus contains a rare allyl side chain, whereas Ascomycin is an ethyl functional group in its place.
The biosynthetic gene clusters of Tacrolimus, Ascomycin and Rapamycin encode a typical type I polyketone synthase (PKS)-non-ribosomal peptide synthase (NRPS) system, which is responsible for the formation of the skeleton lactone ring structure. Tacrolimus, for example, is a twenty-three macrolide containing amide bonds catalyzed by three type I PKS (FkbA,FkbB, FkbC) and one NRPS (FkbP) .
Pharmacological Mechanism of Tacrolimus
Tacrolimus is classical Calcineurin inhibitors (CAI), which belongs to the immunosuppressant characterized by Calcineurin inhibition. Tacrolimus binds intracellular binding protein (FKBP) to form a complex that inhibits T cell activation, TNF-α, IL-1β and IL-6 production, and T cell-dependent B cell proliferation by inhibiting Calcineurin and IL-2 transcription. The effect is similar to that of Cyclosporine. However, studies showed that Tacrolimus inhibits T cell activation more strongly and is more effective than cyclosporine in treating acute rejection.
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