Catalog No.S5004 Synonyms: ASM 981
Molecular Weight(MW): 810.45
Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12 (FKBP-12); a calcineurin inhibitor.
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Pim inhibits nuclear factor of activated T-cell (NFAT) translocation of cultured human vascular smooth muscle cells. hCASM expressing green fluorescent protein-NFAT were incubated with 10 uM Pim for 30 min. Left: mean nuclear/cytosol fluorescence intensity ratio (±SE) is displayed at basal conditions and after stimulation with 500 uM ATP in the absence and presence of Pim.
Am J Physiol Heart Circ Physiol 2013 305(11), H1646-57. Pimecrolimus purchased from Selleck.
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|Description||Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12 (FKBP-12); a calcineurin inhibitor.|
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. 
|In vivo||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. Pimecrolimus shows only a low potential to impair systemic immune responses when compared with tacrolimus as shown in rats in (1) the localized graft-versus-host reaction, (2) the antibody formation to sheep red blood cells, and (3) kidney transplantation.|
|In vitro||DMSO||100 mg/mL (123.38 mM)|
|Ethanol||100 mg/mL (123.38 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02896101||Recruiting||Atopic Dermatitis||Glenmark Pharmaceuticals Ltd. India||August 2016||Phase 3|
|NCT02791308||Active, not recruiting||Atopic Dermatitis||Actavis Inc.||February 2015||Phase 3|
|NCT02376049||Completed||Atopic Dermatitis||LEO Pharma||February 2015||Phase 1|
|NCT02103725||Completed||Atopic Dermatitis||LEO Pharma||April 2014||Phase 1|
|NCT01692626||Unknown status||Rash||Mohammed Almubarak, MD|West Virginia University||February 2012||Phase 2|
|NCT02443311||Completed||Oral Lichen Planus||Ain Shams University||September 2010||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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