吡拉米司特

生物活性靶点体外研究体内研究吡拉米司特试剂级价格

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

吡拉米司特化学性质

沸点 :447.8±45.0 °C(Predicted)
密度 :1.370
储存条件 :2-8°C
溶解度 :DMSO: soluble20mg/mL, clear
酸度系数(pKa) :10.10±0.70(Predicted)
形态 :powder
颜色 :white to beige

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26
WGK Germany :3

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。

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 )

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.

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.