Piclamilast(Synonyms: RP 73401; RPR 73401)

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Piclamilast (Synonyms: RP 73401; RPR 73401)

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。

Piclamilast(Synonyms: RP 73401;  RPR 73401)

Piclamilast Chemical Structure

CAS No. : 144035-83-6

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5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
25 mg ¥5200 In-stock
50 mg ¥8300 In-stock
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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[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 IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[2]

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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

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°C)

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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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.

    [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.

    [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(40):42026-40.

    [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.

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