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  • Pimecrolimus
    • 匹美克莫司;SDZ-ASM 981
    货号: abs813401
    CAS号: 137071-32-0
    分子式: C43H68ClNO11
    分子量: 810.45
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813401-10mg 1-2周 ¥846.00
    - +
    abs813401-25mg 1-2周 ¥1654.00
    - +
    abs813401-50mg 1-2周 ¥2958.00
    - +
    abs813401-100mg 1-2周 ¥5324.00
    - +
    大包装询价
    产品描述
    描述

    Pimecrolimus是一种炎性细胞因子分泌物。

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    匹美克莫司;SDZ-ASM 981
    可溶性/溶解性
    Ethanol :93 mg/mL (114.8 mM)
    DMSO :93 mg/mL (114.8 mM)
    生物活性
    In vitro(体外研究)
    Pimecrolimus blocks T-lymphocyte activation pathway by inhibiting calcineurin function. 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.
    In vivo(体内研究)
    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. 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.
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