Delivery Tacrolimus Powder Purity Tacrolimus Powder Pharmaceutical Tacrolimus
Prouct Description
Product Details
| Product Name |
Tacrolimus |
| Apperance |
White or off-white crystalline powder |
| CAS |
104987-11-3 |
| MF |
C44H69NO12 |
| MW |
804.031 |
Tacrolimus, also known as FK506, is a fermentation product isolated from the Streptomyces genus (streptomycestsukubaensis), and its chemical structure belongs to the 23-molecule macrolide antibiotics. It is a powerful new type of immunosuppressant, mainly by inhibiting the release of interleukin-2 (L-2), comprehensively inhibiting the effect of T lymphocytes, and is 100 times stronger than cyclosporine (CsA).
Application&Function
Manufacturing method
Obtained by fermentation from Streptomyces tsukubaensis. The fermentation process is as follows: Transfer 100 mL of seed solution (containing 1% glycerol, 1% corn starch, 0.5% glucose, 1% cottonseed powder, 0.5% corn impregnation solution and 0.2% calcium carbonate, pH=6.5) into a 500ml bottle and disinfect it at 120ºC for 30 minutes. A circle of seeds of S. sukubaensis No. 9993 cultivated on an inclined plane was inoculated and cultivated at 30ºC for 4 days. Transfer the culture medium into the container containing 201. The same seed liquid was placed in a 30L fermentation tank that had been disinfected at 120ºC for 30 minutes and cultivated at 30ºC for 2 days. Air was blown in at a rate of 2L/min and stirred at a rate of 300r/min. 16L of this culture medium was implanted into a 2000L tank containing 1600L of fermentation solution (containing 4.5% soluble starch, 1% corn maculate solution, 1% dry yeast, 0.1% calcium carbonate and 0.1%Adekancd, pH=6.8) that had been disinfected at 120ºC for 30 minutes. Fermentation was carried out for 4 days at 30ºC, with stirring at 170r/min and air flow at 1600L/min. Separation: Filter 1500L of fermentation broth with the assistance of 25kg of diatomite. The filter cake was extracted with 500L . The extract and filtrate (1350L) were combined and passed through a mixture containing 100L of DiAIon HP-20 nonionic absorption resin (Mitsubishi(2hemical Industries Ltd.). The pillar of "Japan products". After washing with 300L of water and 300L of 50% solution, elute with 75% solution. The eluent was concentrated under reduced pressure to approximately 300L of aqueous solution, and then extracted three times with 20L . The extracts are combined and concentrated under reduced pressure until the remaining oily substances are formed. The oily residue was mixed with twice the weight of acidic silica gel (special silica gelgrade 12, Fuji(9evision Co, Japan product) and then immersed . The solvent was distilled out, and the remaining dry powder was chromatographed with 8L of the same acidic silica gel column. It was eluted with 30L , a mixture of 30L (4:1), and 30L. Collect the eluent containing fujimycin and concentrate it under reduced pressure. Mix the oily residue with twice the weight of acidic silica gel and immerse it . The solvent was distilled out, and the resulting dry powder was chromatographed using a 3.5L acidic silica gel column. It was eluted with 10L, a 10L mixture (4:1), and 10L . Collect the eluent containing fujimycin and concentrate it under reduced pressure. The obtained yellow oily residue was dissolved in a mixture of 300ml (1:1), and 2L of silica gel (230-400μm, Merck Co. Column chromatography was performed using (first 10L 1:1, then 6L 1:2) and 6L for elution. Collect the eluent containing fujimycin, reduce pressure and concentrate it to obtain 34g of white powder fujimycin. Dissolve it and concentrate under reduced pressure. The concentrated solution was placed overnight at 5ºC, resulting in 22.7g of prismatic crystals. Recrystallization with was used again to obtain 13.6g of colorless prismatic crystals of pure fujimycin.
Purpose
1. Macrolide antibiotics. Immunosuppressant. The mechanism of action is the same as that of cyclosporine, mainly inhibiting the synthesis of interleukin-2. Rejection reactions for organ transplantation.
Second, 104987-11-3 (tacrolimus) is the preferred immunosuppressive drug for patients undergoing liver and kidney transplantation. It can also be selected for those who develop rejection reactions after liver and kidney transplantation and are resistant to traditional immunosuppressive regimens.
Third, pharmacological effects At the molecular level, the effect of tacrolimus is clearly achieved by binding to cellular proteins (FKBP12) and accumulating within cells to exert its efficacy. The FKBP12-tacrolimus complex specifically binds to and inhibits calcinurin, which inhibits the calcium ion-dependent signaling pathway produced in T cells, thereby preventing the transcription of discontinuous lymphokine genes. This medicine is a highly immunosuppressive drug, and its activity has been confirmed both in vitro and in vivo experiments. This drug inhibits the production of cytotoxic lymphocytes that cause major transplant rejection. This medicine inhibits the activation of T cells and the proliferation of T helper cells dependent on B cells. It will also inhibit the production of lymphokines such as interleukin-2, interleukin-3 and interferon - γ, as well as the expression of interleukin-2 receptors. At the molecular level, the effect of this drug seems to be produced by binding to the cellular protein (FKBP), which also causes the compound to accumulate between cells. It was found in in vivo experiments that this drug showed effectiveness for liver and kidney transplantation.
Specification
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