吡拉米司特 T23154

Product Introduction
Bioactivity


英文名: Piclamilast

描述: Piclamilast (RP 73401) 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。

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 30 mg/ml(78.69 mM)


关键字: RP73401 | RP-73401 | inhibit | Phosphodiesterase (PDE) | AML | RPR73401 | phosphodiesterase | PDE | Piclamilast | RPR-73401 | RAR | Inhibitor | ATRA | cAMP

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相关库: Anti-Neurodegenerative Disease Compound Library | ReFRAME Related Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Metabolism Compound Library | Anti-Alzheimer's Disease Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途