产品
编 号:F141030
分子式:C43H68ClNO11
分子量:810.45
产品类型
结构图
CAS No: 137071-32-0
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生物活性:
Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity.
体内研究:
Pimecrolimus (SDZ-ASM 981) (0-0.4%; topical; 10 μL once) inhibits allergic contact dermatitis in mice and pigs.Pimecrolimus (0-90 mg/kg; p.o. or s.c.; twice or once) potently inhibits allergic contact dermatitis in mice and rats.Animal Model:Female NMRl mice, allergic contact dermatitis model
Dosage:0.004%, 0.01%, 0.04%, 0.13% and 0.4% in10 μL ethanolic solution
Administration:Topical application, once
Result:Inhibited oedema formation by 17% at concentration of 0.004%.
Animal Model:Female NMRl mice, allergic contact dermatitis model
Dosage:10, 30, 90 mg/kg (oral) or 1.5, 4.5, 13.5 mg/kg (subcutaneous)
Administration:Oral (twice) or subcutaneous administration (once)
Result:Signiticantiy inhibited inflammatory ear oedema formation.
体外研究:
Pimecrolimus (SDZ-ASM 981) (100 nM) targets T-cells and mast cells and inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals essential for the activation of inflammatory T-lymphocytes.Pimecrolimus acts specifically on cells that are crucial for the effector phase of an inflammatory reaction.Pimecrolimus (10 nM; 3 days) inhibits the polyclonal growth of peripheral blood T cells in murine and human mixed lymphocyte reactions.Pimecrolimus inhibits cytokine IL-2, IL-4, IL-10 and interferon-γ release from T-cell clone CFTS4:3.1 with IC50s of 0.28, 0.3, 0.2 and 0.42 nM, respectively after antigen-specific stimulation.