144035-83-6
基本信息
RPR 73401
piclamilas
Piclamilast
N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide
3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide
3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide
3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide
Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-
物理化学性质
| 沸点 | 447.8±45.0 °C(Predicted) |
| 密度 | 1.370 |
| 储存条件 | 2-8°C |
| 溶解度 | 在DMSO中的溶解度为20mg/mL，澄清 |
| 酸度系数(pKa) | 10.10±0.70(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H315-H319-H335 |
| 防范说明 | P261-P264-P271-P280-P302+P352-P305+P351+P338 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 26 |
| WGK Germany | 3 |
常见问题列表
|
PDE4 16 nM (IC 50 , in pig aorta) |
PDE4 2 nM (IC 50 , in eosinophil soluble) |
PDE1 >100 μM (IC 50 ) |
PDE2 40 μM (IC 50 ) |
PDE3 >100 μM (IC 50 ) |
PDE5 14 μM (IC 50 ) |
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 IC
50
values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively.
RT-PCR
| Cell Line: | Human A549 type II lung epithelial cells. |
| Concentration: | 1 μM (H 2 O 2 200 μM). |
| Incubation Time: | 30 min. |
| Result: | Prevented H 2 O 2 -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. |
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.
| 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. |