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Pimecrolimus

Name: Pimecrolimus
Brand: Selleck Chemicals
SKU: S5004
Rating: 5 (14 reviews)

Synonyms: Elidel,SDZ-ASM 981

Catalog No.S5004 Purity: 99.87%

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: 137071-32-0

Selleck's Pimecrolimus has been cited by 14 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.87%

99.87

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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
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]
Cell Research	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.

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05439941	Terminated	Atopic Dermatitis	Evelo Biosciences Inc.	June 6 2022	Phase 2
NCT01692626	Terminated	Rash	West Virginia University	February 2012	Phase 2
NCT00507832	Completed	Prurigo Nodularis	University Hospital Muenster\|Novartis Pharmaceuticals	April 2007	Phase 2
NCT00208026	Completed	Netherton Syndrome	Children''s Hospital of Philadelphia\|Novartis Pharmaceuticals	September 2005	Phase 1\|Phase 2

References

[4] Xu P, et al. Korean J Physiol Pharmacol. 2017, 21(3):287-292.

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Chemical lnformation & Solubility

Molecular Weight	810.45	Formula	C₄₃H₆₈ClNO₁₁
CAS No.	137071-32-0	SDF	Download Pimecrolimus SDF
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
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (123.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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