Piclamilast 是一种有效的磷酸二酯酶 4(PDE4)的抑制剂，对猪主动脉和可溶性嗜酸性粒细胞中的IC50值分别为 16 nM 和 2 nM。

Piclamilast is a PDE4 inhibitor.

Piclamilast pre-treatment significantly inhibited the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63[1]. The IC50s for Piclamilast was 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively. Piclamilast exhibited IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].

Initial in vivo studies conducted in severe combined immunodeficiency mice transplanted with NB4 leukemia cells indicate that the enhancing effect of piclamilast on ATRA-induced myeloid maturation translates into a therapeutic benefit[2].

144035-83-6

C18H18Cl2N2O3

381.25

吡拉米司特;RPR 73401;RP 73401;Piclamilast

DMSO:30 mg/ml(78.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years