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CAS No. : 144035-83-6
MCE 国际站:Piclamilast
产品活性:Piclamilast (RP 73401) 是有效的磷酸二酯酶 4 (PDE4) 的抑制剂,其在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。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphodiesterase (PDE)
In Vitro: Piclamilast (RP 73401, 1 μM, 30 min) significantly inhibits the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63.
Piclamilast (RP 73401) exhibits IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively.
In Vivo: Piclamilast (RP 73401, 10 mg/kg, 30 min) alone does not affect the MST of leukemia-bearing animals. Piclamilast combined with ATRA (HY-14649) significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.
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