Pimecrolimus

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

Validation & Quality Control

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Quality Control & MSDS

Related Compound Libraries

Pimecrolimus is available in the following compound libraries:

Product Information

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)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02103725 Active, not recruiting Atopic Dermatitis LEO Pharma April 2014 Phase 1
NCT01692626 Recruiting Rash Mohammed Almubarak, MD|West Virginia University February 2012 Phase 2
NCT01202149 Completed Eczema|Atopic Dermatitis Frankel, Amylynne, M.D.|Onset Therapeutics, Inc March 2010 Phase 4
NCT01082393 Recruiting Vitiligo University Hospital, Ghent February 2010 Phase 4
NCT00946478 Completed Atopic Dermatitis University of California, San Diego|Novartis October 2009 --

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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

Customer Reviews (1)


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Rating
Source Am J Physiol Heart Circ Physiol 2013, 305(11):H1646-57. Pimecrolimus purchased from Selleck
Method NFAT translocation
Cell Lines Human vascular smooth muscle cells
Concentrations 10 uM
Incubation Time 30 min
Results Pimecrolimus, lacks inhibitory effects on calcineurin, suppression of NFAT translocation was predominantly expected for pimecrolimus. ATP-induced NFAT nuclear translocation was strongly suppressed by 30-min preincubation with pimecrolimus.

Product Citations (2)

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