吡拉米司特
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- CAS号:
- 144035-83-6
- 英文名:
- Piclamilast
- 英文别名:
- RP 73401;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-;inhibit,Phosphodiesterase (PDE),RPR73401,AML,phosphodiesterase,PDE,RAR,RP-73401,Inhibitor,Piclamilast,RP73401,RPR-73401,ATRA,cAMP
- 中文名:
- 吡拉米司特
- 中文别名:
- PICLAMILAST,PDE4抑制剂
- CBNumber:
- CB51328847
- 分子式:
- C18H18Cl2N2O3
- 分子量:
- 381.25
- MOL File:
- 144035-83-6.mol
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吡拉米司特化学性质
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沸点:
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447.8±45.0 °C(Predicted)
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密度:
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1.370
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble20mg/mL, clear
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酸度系数(pKa):
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10.10±0.70(Predicted)
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形态:
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powder
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颜色:
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white to beige
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吡拉米司特性质、用途与生产工艺
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。
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PDE4
16 nM (IC
50
, in pig aorta)
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PDE4
2 nM (IC
50
, in eosinophil soluble)
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PDE1
>100 μM (IC
50
)
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PDE2
40 μM (IC
50
)
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PDE3
>100 μM (IC
50
)
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PDE5
14 μM (IC
50
)
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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
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Cell Line:
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Human A549 type II lung epithelial cells.
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Concentration:
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1 μM (H
2
O
2
200 μM).
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Incubation Time:
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30 min.
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Result:
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Prevented H
2
O
2
-induced changes in gene expression levels in A549 cells.
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Cell Viability Assay
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Cell Line:
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NB4 cells.
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Concentration:
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30 μM.
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Incubation Time:
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3 days.
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Result:
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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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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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Animal Model:
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SCID mice.
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Dosage:
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10 mg/kg (combined with ATRA (HY-14649)).
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Administration:
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Injection daily.
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Result:
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Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.
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吡拉米司特
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
吡拉米司特
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吡拉米司特国内生产厂家
144035-83-6, 吡拉米司特 相关搜索:
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- Aromatics
- 合成有机化合物配体
- PICLAMILAST,PDE4抑制剂
- 144035-83-6
- inhibit,Phosphodiesterase (PDE),RPR73401,AML,phosphodiesterase,PDE,RAR,RP-73401,Inhibitor,Piclamilast,RP73401,RPR-73401,ATRA,cAMP
- piclamilas
- 3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide
- Piclamilast
- N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide
- 3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide
- 3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide
- RPR 73401
- RP 73401
- Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-