Pimecrolimus

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

与所有子囊霉素一样，吡美莫司是一种亲免素配体，可与胞质受体、亲免素巨噬蛋白-12 特异性结合。

Pimecrolimus, like all ascomycins, is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.(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.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.(In Vivo):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.

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.Cell Proliferation Assay Cell Line:T-cell clone (TCC), murine and human mixed lymphocyte reactions (MLR)Concentration:0-10 nM Incubation Time:3 days Result:Inhibited proliferation of TCC CFTS 4:3.1 with IC50s of 0.78-2.6 nM. Inhibited murine and human MLR with IC50s of both 1.3 nM.

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.

Elidel | SDZ-ASM 981

Others

Other Targets

Others

Inflammation/Immunology

——

137071-32-0

810.45

C43H68ClNO11

>98% (HPLC)

Ethanol: 100 mg/mL (123.38 mM); DMSO: 100 mg/mL (123.38 mM)

O=C(C(N1CCCC[C@@]1([H])C(O[C@H](/C(C)=C/[C@H]2C[C@@H](OC)[C@@H](Cl)CC2)[C@H](C)[C@@H](O)C3)=O)=O)[C@@](O4)(O)[C@H](C)C[C@H](OC)[C@@]4([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@@H](CC)C3=O

(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-12-[(1E)-2{(1R,3R,4S)-4-chloro-3-methoxycyclohexyl}-1-methylvinyl]-17-ethyl-1,14-dihydroxy-23,25 dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-aza-tricyclo[22.3.1.0 4,9]octacos-18-ene2,3,10,16-tetraone.

(-20℃)

With Ice Pack

≥ 2 years