| Bioactivity | Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity[1][2]. | ||||||||||||
| Target | Calcineurin | ||||||||||||
| Invitro | 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]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | Pimecrolimus | ||||||||||||
| CAS | 137071-32-0 | ||||||||||||
| Formula | C43H68ClNO11 | ||||||||||||
| Molar Mass | 810.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Grassberger M, et al. Pimecrolimus -- an anti-inflammatory drug targeting the skin. Exp Dermatol. 2004 Dec;13(12):721-30. [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. [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. |
Pimecrolimus
CAS: 137071-32-0 F: C43H68ClNO11 W: 810.45
Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrol
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