吡拉米司特
| 中文名称 | 吡拉米司特 |
|---|---|
| 中文同义词 | PICLAMILAST,PDE4抑制剂 |
| 英文名称 | Piclamilast |
| 英文同义词 | Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-;RP 73401;RPR 73401;3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide;3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide;N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide;Piclamilast;3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide |
| CAS号 | 144035-83-6 |
| 分子式 | C18H18Cl2N2O3 |
| 分子量 | 381.25 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 144035-83-6.mol |
| 结构式 |  |
吡拉米司特 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 |
|
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. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12887 | 吡拉米司特 Piclamilast | 144035-83-6 | 5 mg | 1500元 |
| 2024/04/30 | HY-12887 | 吡拉米司特 Piclamilast | 144035-83-6 | 10 mg | 2400元 |