Pimecrolimus

Catalog No.S5004 Synonyms: ASM 981

Pimecrolimus Chemical Structure

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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Biological Activity

Description Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12 (FKBP-12); a calcineurin inhibitor.
In vitro

Pimecrolimus blocks T-lymphocyte activation pathway by inhibiting calcineurin function. [1] 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. [2]

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. [2] 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.[3]

Protocol

Cell Research:

[4]

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  • Cell lines: melanocytes
  • Concentrations: 1, 10, 100, 1,000 nM
  • Incubation Time: 3 days
  • Method:

    The proliferation rate of melanocytes was determined using a colorimetric MTT assay. Melanocytes were plated in 96-well microplates, and each well was pretreated with 100 µl of different concentrations (1, 10, 100, 1,000 nM) of pimecrolimus for 3 days. Then, 50 µL of 5 mg/mL 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) solution was added to each well. The resulting formazan was dissolved with 150 µL dimethylsulfoxide. The absorbance of the samples was measured at a wavelength of 490 nm.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (123.38 mM)
Ethanol 100 mg/mL (123.38 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 810.45
Formula

C43H68ClNO11

CAS No. 137071-32-0
Storage powder
Synonyms ASM 981

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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

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID