Pimecrolimus

Catalog No.S5004 2 Product Citations

Pimecrolimus, like all ascomycins, is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.

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Pimecrolimus Chemical Structure

Pimecrolimus Chemical Structure
Molecular Weight: 810.45

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Product Description

Biological Activity

Description Pimecrolimus, like all ascomycins, is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
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]
Features

Protocol(Only for Reference)

1

References

[1] Nghiem P, et al. Am Acad Dermatol, 2002, 46(2), 228-241.

[2] Gupta AK, et al. J Eur Acad Dermatol Venereol, 2003, 17(5), 493-503.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01037881 Completed Atopic Dermatitis LEO Pharma 2009-12 Phase 2
NCT01082393 Recruiting Vitiligo University Hospital, Ghent 2010-02 Phase 4
NCT01202149 Completed Eczema|Atopic Dermatitis Frankel, Amylynne, M.D.|Onset Therapeutics, Inc 2010-03 Phase 4
NCT01692626 Recruiting Rash West Virginia University|Mohammed Almubarak, MD 2012-02 Phase 2
NCT02103725 Not yet recruiting Atopic Dermatitis LEO Pharma 2014-04 Phase 1

Chemical Information

Download Pimecrolimus SDF
Molecular Weight (MW) 810.45
Formula

C43H68ClNO11

CAS No. 137071-32-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms ASM 981
Solubility (25°C) * In vitro DMSO 162 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 162 mg/mL (199 mM)
* <1 mg/ml means slightly soluble or 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 Name 15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-[(1E)-2-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]-1-methylethenyl]-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-, (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-

Research Area

Product Citations (2)

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