Pimecrolimus Chemical Structure

Pimecrolimus Chemical Structure
Molecular Weight: 810.45

Validation & Quality Control

Customer Reviews(1)

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.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-12-20)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02103725 Completed Atopic Dermatitis LEO Pharma April 2014 Phase 1
NCT02103725 Completed Atopic Dermatitis LEO Pharma April 2014 Phase 1
NCT01692626 Recruiting Rash Mohammed Almubarak, MD|West Virginia University February 2012 Phase 2
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

view more

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 solvent (DMSO, water, etc.)
Synonyms ASM 981
Solubility (25°C) * In vitro DMSO 162 mg/mL (199.88 mM)
Water <1 mg/mL (<1 mM)
Ethanol 162 mg/mL (199.88 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)


Click to enlarge
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)

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:2

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Others Products

  • (S)-crizotinib

    (S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM.

  • PTC-209

    PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).

  • KN-93 Phosphate

    KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.

  • CX-4945 (Silmitasertib)

    CX-4945 (Silmitasertib) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2.

    Features:First clinical inhibitor of CK2.

  • Tacrolimus (FK506)

    FK-506 is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.

  • Bendamustine HCl

    Bendamustine HCL is a DNA-damaging agent with IC50 of 50 μM.

  • Cyclophosphamide Monohydrate

    Cyclophosphamide Monohydrate is a nitrogen mustard alkylating agent, it attaches the alkyl group to the guanine base of DNA.

  • Cabazitaxel

    Cabazitaxel (XRP6258) is a semi-synthetic derivative of a natural taxoid.

    Features:A semi-synthetic derivative of a natural taxoid.

  • Verteporfin

    Verteporfin is a potent second-generation photosensitizing agent derived from porphyrin.

  • Cyclosporin A

    Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM, widely used in organ transplantation to prevent rejection.

Recently Viewed Items

Tags: buy Pimecrolimus | Pimecrolimus ic50 | Pimecrolimus price | Pimecrolimus cost | Pimecrolimus solubility dmso | Pimecrolimus purchase | Pimecrolimus manufacturer | Pimecrolimus research buy | Pimecrolimus order | Pimecrolimus mouse | Pimecrolimus chemical structure | Pimecrolimus mw | Pimecrolimus molecular weight | Pimecrolimus datasheet | Pimecrolimus supplier | Pimecrolimus in vitro | Pimecrolimus cell line | Pimecrolimus concentration | Pimecrolimus nmr
Contact Us