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Piclamilast

Catalog No. T23154 CAS 144035-83-6

Synonyms: RPR 73401, RP 73401

Piclamilast (RP 73401) is a PDE4 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Piclamilast, CAS 144035-83-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 428.00
50 mg	In stock	$ 639.00
100 mg	In stock	$ 890.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Piclamilast (RP 73401) is a PDE4 inhibitor.
Targets&IC50	PDE2:40 μM, PDE3:>100 μM, PDE5:14 μM, PDE1:>100 μM, PDE4:16 nM (pig aorta), PDE4:2 nM (eosinophil soluble)
In vitro	Piclamilast pre-treatment significantly inhibited the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63[1]. The IC50s for Piclamilast was 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively. Piclamilast exhibited IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].
In vivo	Initial in vivo studies conducted in severe combined immunodeficiency mice transplanted with NB4 leukemia cells indicate that the enhancing effect of piclamilast on ATRA-induced myeloid maturation translates into a therapeutic benefit[2].

Synonyms	RPR 73401, RP 73401
Molecular Weight	381.25
Formula	C18H18Cl2N2O3
CAS No.	144035-83-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/ml(78.69 mM)

References and Literature

1. 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. 2. 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. 3. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Inhibitor Library ReFRAME Related Library Bioactive Compounds Library Max Bioactive Compound Library Metabolism Compound Library Anti-Alzheimer's Disease Compound Library Human Metabolite Library

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Related compounds with same targets

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Piclamilast 144035-83-6 Metabolism PDE RPR 73401 RP73401 RP-73401 inhibit Phosphodiesterase (PDE) AML RPR73401 phosphodiesterase RP 73401 RPR-73401 RAR Inhibitor ATRA cAMP inhibitor

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