Pimecrolimus

Catalog No.S5004 Synonyms: Elidel,SDZ-ASM 981

For research use only.

Pimecrolimus (Elidel,ASM 981,SDZ-ASM 981) is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12 (FKBP-12); a calcineurin inhibitor.

Pimecrolimus Chemical Structure

CAS No. 137071-32-0

Selleck's Pimecrolimus has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description Pimecrolimus (Elidel,ASM 981,SDZ-ASM 981) 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 (from reference)

Cell Research:

[4]

  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 810.45
Formula

C43H68ClNO11

CAS No. 137071-32-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1C=C(CC(CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC1=O)O)C)C(=CC4CCC(C(C4)OC)Cl)C)O)C)OC)OC)C)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05439941 Enrolling by invitation Drug: EDP1815 Atopic Dermatitis Evelo Biosciences Inc. June 6 2022 Phase 2
NCT01692626 Terminated Drug: Pimecrolimus|Drug: Placebo Rash West Virginia University February 2012 Phase 2
NCT00507832 Completed Drug: Pimecrolimus|Drug: Hydrocortisone Prurigo Nodularis University Hospital Muenster|Novartis Pharmaceuticals April 2007 Phase 2
NCT00208026 Completed Drug: Pimecrolimus 1% Cream Netherton Syndrome Children''s Hospital of Philadelphia|Novartis Pharmaceuticals September 2005 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

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