Piclamilast

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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。

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°C	3 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	2.6230 mL	13.1148 mL	26.2295 mL
5 mM	0.5246 mL	2.6230 mL	5.2459 mL
10 mM	0.2623 mL	1.3115 mL	2.6230 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。