Pimecrolimus

製品コードS5004 バッチS500405

印刷

化学情報

Synonyms

Elidel,SDZ-ASM 981

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₄₃H₆₈ClNO₁₁

分子量

810.45

CAS No.

137071-32-0

Solubility (25°C)*

体外

DMSO

100 mg/mL (123.38 mM)

Ethanol

25 mg/mL (30.84 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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] This compound prevents the release of cytokines and pro-inflammatory mediators from mast cells. It 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. This chemical 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. This 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. This compound 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] It is as effective as the high-potency corticosteroid clobetasol-17-propionate in a pig model of allergic contact dermatitis (ACD). This chemical also effectively reduces skin inflammation and pruritus in hypomagnesemic hairless rats, a model that mimics acute signs of atopic dermatitis. It 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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	melanocytes
	濃度	1, 10, 100, 1,000 nM
	反応時間	3 days
	実験の流れ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/11807435/
https://pubmed.ncbi.nlm.nih.gov/12941081/
https://pubmed.ncbi.nlm.nih.gov/11770910/

https://pubmed.ncbi.nlm.nih.gov/28461770/

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カスタマーフィードバック

: Data from [Am J Physiol Heart Circ Physiol, 2013, 305(11), H1646-57]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258]	PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y]	PubMed: 35118583
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918]	PubMed: 34383271
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4]	PubMed: 34731453
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z]	PubMed: 34304386
Calcineurin phosphatase activity regulates Varicella-Zoster Virus induced cell-cell fusion [ PLoS Pathog, 2020, 16(11):e1009022]	PubMed: 33216797
Identification of amitriptyline HCl, flavin adenine dinucleotide, azacitidine and calcitriol as repurposing drugs for influenza A H5N1 virus-induced lung injury. [ PLoS Pathog, 2020, 16;16(3):e1008341]	PubMed: 32176725
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58]	PubMed: 32099531
Establishment and characterization of NCC-MFS2-C1: a novel patient-derived cancer cell line of myxofibrosarcoma [ Hum Cell, 2020, 10.1007/s13577-020-00420-z]	PubMed: 32870449

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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