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Piclamilast

(Synonyms: RP 73401; RPR 73401)

目录号: PC12593 纯度: ≥98%

PDE4抑制剂，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。

CAS No. :144035-83-6

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中文名称

Piclamilast

中文别名

吡拉米司特

英文名称

Piclamilast

英文别名

Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-;Piclamilast;3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide;3-cyclopentyloxy-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide;Cpodpmb;3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-benzamide;N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide;RP 73-401;RP 73401;RPR 73401;3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide

Cas No.

144035-83-6

分子式

C₁₈H₁₈N₂O₃Cl₂

分子量

381.25

包装储存

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

详情描述

PDE4抑制剂，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 a phosphodiesterase 4 (PDE4) inhibitor, with IC₅₀ values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.

性状

Solid

IC50 & Target[1][2]

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.
Piclamilast (RP 73401) exhibits IC₅₀ values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	Human A549 type II lung epithelial cells.
Concentration:	1 μM (H₂O₂ 200 μM).
Incubation Time:	30 min.
Result:	Prevented H₂O₂ -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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

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

参考文献

[1]. M J Ashton, et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. J Med Chem. 1994 May 27;37(11):1696-703. [Information]

[2]. Manuel Mata, et al. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation. Free Radic Res. 2012 May;46(5):690-9. [Information]

[3]. Edoardo Parrella, et al. Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways. J Biol Chem . 2004 Oct 1;279(4 [Information]

[4]. T Ukita, et al. Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. J Med Chem. 1999 Mar 25;42(6):1088-99. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. M J Ashton, et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. J Med Chem. 1994 May 27;37(11):1696-703. [Information]

[2]. Manuel Mata, et al. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation. Free Radic Res. 2012 May;46(5):690-9. [Information]

[3]. Edoardo Parrella, et al. Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways. J Biol Chem . 2004 Oct 1;279(4 [Information]

[4]. T Ukita, et al. Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. J Med Chem. 1999 Mar 25;42(6):1088-99. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Piclamilast

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