Piclamilast

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

Piclamilast 是一种 PDE4 抑制剂。

Piclamilast is a PDE4 inhibitor.(In Vitro):Piclamilast pre-treatment significantly inhibited the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63. 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.(In Vivo):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.

RT-PCR Cell Line:Human A549 type II lung epithelial cells.Concentration:1 μM (H2O2 200 μM).Incubation Time:30 min.Result:Prevented H2O2 -induced changes in gene expression levels in A549 cells.Cell Viability Assay Cell Line:NB4 cells.Concentration:30 μM.Incubation Time:3 days.Result:Exerted a significant enhancing effect on the induction of STAT1 observed in ATRA-treated NB4 cells.Caused a significant increase in the number of cells expressing NBT-R activity.

Animal Model:SCID mice.Dosage:10 mg/kg (combined with ATRA (HY-14649)).Administration:Injection daily.Result:Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

RP 73401 | RPR 73401

Angiogenesis

PDE

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144035-83-6

381.25

C18H18Cl2N2O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (131.15 mM)

COc1ccc(cc1OC1CCCC1)C(=O)Nc1c(Cl)cncc1Cl

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(-20℃)

With Ice Pack

≥ 2 years