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KI0907Pimecrolimus10 mg$176

Chemical Characteristic

Product NamePimecrolimus
SynonymsElidel, ASM 981
CAS No.137071-32-0
Molecular Weight 810.45
FormulaC43H68ClNO11
Chemical Structure

Biological activities

Pimecrolimus is a cell-selective inhibitor of inflammatory cytokines. Pimecrolimus has been specifically developed for the treatment of inflammatory skin diseases, such as atopic dermatitis, and plaque-type psoriasis. Pimecrolimus inhibits the production of inflammatory cytokines in T cells and mast cells and prevents the release of preformed inflammatory mediators from mast cells. Pimecrolimus inhibits the growth of 3 different cell lines (the human keratinocyte line HaCaT, the melanoma cell line G361 and the umbilical vein endothelial line ECV-304) with IC50 range from 3.5 to 7 µM.[1] Pimecrolimus inhibits Th1 cytokine synthesis and also prevents the up-regulation of the OX40 co-receptor on primed T cells. Pimecrolimus inhibits the up-regulation of CD134, CD25 and CD54 expression with IC50 of 10, 1 and 0.1 nM, respectively. Pimecrolimus also inhibits T cell proliferation stimulated by allogeneic DC with an IC50 of 0.55 nM.[2] Pimecrolimus effectively reduces skin inflammation and pruritus in hypomagnesemic hairless rats.[1]

References

[1] Stuetz A, et al. Pimecrolimus (Elidel, SDZ ASM 981)- preclinical pharmacologic profile and skin selectivity. Semin Cutan Med Surg. 2001, 20(4): 233-241. 閵嗏偓閵嗏偓
[2] Kalthoff FS, et al. Pimecrolimus inhibits up-regulation of OX40 and synthesis of inflammatory cytokines upon secondary T cell activation by allogeneic dendritic cells. Clin Exp Immunol. 2002, 130(1): 85-92. 閵嗏偓閵嗏偓

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