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Pimecrolimus

MCE China：Pimecrolimus

Brand：MedChemExpress (MCE)

Cat. No.HY-13723

CAS：137071-32-0

Synonyms：SDZ-ASM 981

Purity：99.53%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity.

In Vitro：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[1]. Pimecrolimus acts specifically on cells that are crucial for the effector phase of an inflammatory reaction[1]. Pimecrolimus (10 nM; 3 days) inhibits the polyclonal growth of peripheral blood T cells in murine and human mixed lymphocyte reactions[2]. 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[2].

In Vivo：Pimecrolimus (SDZ-ASM 981) (0-0.4%; topical; 10 μL once) inhibits allergic contact dermatitis in mice and pigs[3]. Pimecrolimus (0-90 mg/kg; p.o. or s.c.; twice or once) potently inhibits allergic contact dermatitis in mice and rats[3].

IC50 & Target：Calcineurin[1] In Vitro 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[1]. Pimecrolimus acts specifically on cells that are crucial for the effector phase of an inflammatory reaction[1]. Pimecrolimus (10 nM; 3 days) inhibits the polyclonal growth of peripheral blood T cells in murine and human mixed lymphocyte reactions[2]. 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[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Pimecrolimus Related Antibodies Cell Proliferation Assay[2] Cell Line: T-cell clone (TCC), murine and human mixed lymphocyte reactions (MLR)

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References：

[1]. Grassberger M, et al. Pimecrolimus -- an anti-inflammatory drug targeting the skin. Exp Dermatol. 2004 Dec;13(12):721-30.  [Content Brief]

[2]. Grassberger M, et al. A novel anti-inflammatory drug, SDZ ASM 981, for the treatment of skin diseases: in vitro pharmacology. Br J Dermatol. 1999 Aug;141(2):264-73.  [Content Brief]

[3]. Meingassner JG, et al. A novel anti-inflammatory drug, SDZ ASM 981, for the topical and oral treatment of skin diseases: in vivo pharmacology. Br J Dermatol. 1997 Oct;137(4):568-76.  [Content Brief]