Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Piclamilast
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DC Chemicals Limited
China
Product Name: Piclamilast
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ShangHai DC Chemicals Co.,Ltd
China
Product Name: Piclamilast
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 3-(CYCLOPENTYLOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-METHOXYBENZAMIDE
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144035-83-6

144035-83-6 structure

144035-83-6 structure

Name: Piclamilast
Chemical Name: piclamilast
CAS Number: 144035-83-6
Molecular Formula: C₁₈H₁₈Cl₂N₂O₃
Molecular Weight: 381.253
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2017-08-11 16:38:12
Modify Date: 2024-01-08 16:37:49
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].

Name	piclamilast
Synonyms	3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide 3-cyclopentyloxy-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide Piclamilast 3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide Cpodpmb Benzamide, 3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy- 3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology
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)
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]. 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.
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.
References	[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.

Density	1.4±0.1 g/cm3
Boiling Point	447.8±45.0 °C at 760 mmHg
Molecular Formula	C₁₈H₁₈Cl₂N₂O₃
Molecular Weight	381.253
Flash Point	224.6±28.7 °C
Exact Mass	380.069458
PSA	63.68000
LogP	5.25
Vapour Pressure	0.0±1.1 mmHg at 25°C
Index of Refraction	1.626

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
Hazard Codes	Xi
RIDADR	NONH for all modes of transport

22889-78-7 structure

22889-78-7

144036-19-1 structure

144036-19-1

~85%

144035-83-6 structure

144035-83-6

Literature: Cook, David C.; Jones, Ronald H.; Kabir, Humayun; Lythgoe, David J.; McFarlane, Ian M.; Pemberton, Clive; Thatcher, Alan A.; Thompson, David M.; Walton, John B. Organic Process Research and Development, 1998 , vol. 2, # 3 p. 157 - 168

67387-76-2 structure

67387-76-2

~%

144035-83-6 structure

144035-83-6

Literature: Journal of Medicinal Chemistry, , vol. 37, # 11 p. 1696 - 1703

144036-17-9 structure

144036-17-9

~%

144035-83-6 structure

144035-83-6

Literature: Journal of Medicinal Chemistry, , vol. 37, # 11 p. 1696 - 1703

621-59-0 structure

621-59-0

~%

144035-83-6 structure

144035-83-6

Literature: Journal of Medicinal Chemistry, , vol. 37, # 11 p. 1696 - 1703

137-43-9 structure

137-43-9

~%

144035-83-6 structure

144035-83-6

Literature: Journal of Medicinal Chemistry, , vol. 37, # 11 p. 1696 - 1703

Precursor 6
22889-78-7 144036-19-1 67387-76-2 144036-17-9
621-59-0 137-43-9
DownStream 0