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Piclamilast
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Piclamilast图片
CAS NO:144035-83-6
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
RP 73401
RPR 73401
产品介绍
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。
生物活性

Piclamilast (RP 73401) is aphosphodiesterase4 (PDE4)inhibitor, withIC50values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively[1][2][3][4].

IC50& Target

PDE4

16 nM (IC50, in pig aorta)

PDE4

2 nM (IC50, in eosinophil soluble)

PDE1

>100 μM (IC50)

PDE2

40 μM (IC50)

PDE3

>100 μM (IC50)

PDE5

14 μM (IC50)

体外研究
(In Vitro)

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[2].
Piclamilast (RP 73401) exhibits IC50values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].

RT-PCR[2]

Cell Line:Human A549 type II lung epithelial cells.
Concentration:1 μM (H2O2200 μM).
Incubation Time:30 min.
Result:Prevented H2O2-induced changes in gene expression levels in A549 cells.

Cell Viability Assay[3]

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
(In Vivo)

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[3].

Animal Model:SCID mice[3].
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.
分子量

381.25

性状

Solid

Formula

C18H18Cl2N2O3

CAS 号

144035-83-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(87.42 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6230 mL13.1148 mL26.2295 mL
5 mM0.5246 mL2.6230 mL5.2459 mL
10 mM0.2623 mL1.3115 mL2.6230 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。