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Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
Pimecrolimus blocks T-lymphocyte activation pathway by inhibiting calcineurin function. Pimecrolimus prevents the release of cytokines and pro-inflammatory mediators from mast cells. Pimecrolimus binds to macrophilin-12, the pimecrolimusmacrophilin complex then binds to the cytosolic enzyme calcineurin phosphatase. The pimecrolimus-macrophilin complex prevents the dephosphorylation of the cytoplasmic component of the nuclear factor of activated T cells by inhibiting the action of calcineurin. Pimecrolimus inhibits not only the transcription and synthesis of cytokines from mast cells, but also the release of preformed mediators serotonin and β-hexosaminidase by the inhibition of Fc∈-RI-mediated degranulation and secretion. Pimecrolimus treatment causes a strong down-regulation of the expression of mRNA for genes associated with the macrolactam target pathway and inflammation.
Pimecrolimus is found to be as effective as cyclosporine A following oral ingestion and slightly superior after subcutaneous administration in mice. Pimecrolimus contrasts cyclosporine A and tacrolimus by inhibiting ongoing secondary inflammatory response, but not impairing the primary immune response in allergic contact dermatitis in mice. Pimecrolimus is as effective as the high-potency corticosteroid clobetasol-17-propionate in a pig model of allergic contact dermatitis (ACD). Pimecrolimus also effectively reduces skin inflammation and pruritus in hypomagnesemic hairless rats, a model that mimics acute signs of atopic dermatitis . For the detailed information of Pimecrolimus, the solubility of Pimecrolimus in water, the solubility of Pimecrolimus in DMSO, the solubility of Pimecrolimus in PBS buffer, the animal experiment (test) of Pimecrolimus, the cell expriment (test) of Pimecrolimus, the in vivo, in vitro and clinical trial test of Pimecrolimus, the EC50, IC50,and affinity,of Pimecrolimus, For the detailed information of Pimecrolimus, the solubility of Pimecrolimus in water, the solubility of Pimecrolimus in DMSO, the solubility of Pimecrolimus in PBS buffer, the animal experiment (test) of Pimecrolimus, the cell expriment (test) of Pimecrolimus, the in vivo, in vitro and clinical trial test of Pimecrolimus, the EC50, IC50,and affinity,of Pimecrolimus, Please contact DC Chemicals. |
