吡拉米司特
- CAS号:144035-83-6
- 英文名:Piclamilast
- 中文名:吡拉米司特
- CBNumber:CB51328847
- 分子式:C18H18Cl2N2O3
- 分子量:381.25
- MOL File:144035-83-6.mol
- 沸点 :447.8±45.0 °C(Predicted)
- 密度 :1.370
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble20mg/mL, clear
- 酸度系数(pKa) :10.10±0.70(Predicted)
- 形态 :powder
- 颜色 :white to beige
吡拉米司特性质、用途与生产工艺
- 生物活性 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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靶点
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 )
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体外研究
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.
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体内研究
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：2024/11/08
- 产品编号：HY-12887
- 产品名称：Piclamilast
- CAS编号：
- 包装：1 mg
- 价格：490元
- 更新日期：2024/11/08
- 产品编号：HY-12887
- 产品名称：吡拉米司特 Piclamilast
- CAS编号：144035-83-6
- 包装：5 mg
- 价格：1200元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
