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。
| 生物活性 | Piclamilast (RP 73401) is aphosphodiesterase4 (PDE4)inhibitor, withIC50values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively[1][2][3][4]. |
| IC50& Target | PDE4 16 nM (IC50, in pig aorta) | PDE4 2 nM (IC50, in eosinophil soluble) | PDE1 >100 μM (IC50) | PDE2 40 μM (IC50) | PDE3 >100 μM (IC50) | PDE5 14 μM (IC50) |
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体外研究
(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[2].
Piclamilast (RP 73401) exhibits IC50values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].
RT-PCR[2] | Cell Line: | Human A549 type II lung epithelial cells. | | Concentration: | 1 μM (H2O2200 μM). | | Incubation Time: | 30 min. | | Result: | Prevented H2O2-induced changes in gene expression levels in A549 cells. |
Cell Viability Assay[3] | 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.
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体内研究
(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[3].
| Animal Model: | SCID mice[3]. | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(87.42 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6230 mL | 13.1148 mL | 26.2295 mL | | 5 mM | 0.5246 mL | 2.6230 mL | 5.2459 mL | | 10 mM | 0.2623 mL | 1.3115 mL | 2.6230 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
