Piclamilast

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Cat.No. 4525 - Piclamilast | C18H18Cl2N2O3 | CAS No. 144035-83-6
Description: Potent and selective PDE4 inhibitor
Alternative Names: RP 73401
Chemical Name: 3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective inhibitor of phosphodiesterase (PDE) 4 (IC50 = 1 nM at PDE4 from human neutrophils). Displays >19,000-fold selectivity over other PDE isoenzymes. Exhibits anti-inflammatory effects in models of allergic inflammation. Also inhibits LTB4 synthesis in human neutrophils (IC50 = 2 nM).

Compound Libraries

Piclamilast is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 381.25
Formula C18H18Cl2N2O3
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 144035-83-6
PubChem ID 154575
InChI Key RRRUXBQSQLKHEL-UHFFFAOYSA-N
Smiles O=C(NC3=C(Cl)C=NC=C3Cl)C1=CC(OC2CCCC2)=C(OC)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.12 100
ethanol 7.62 20

Preparing Stock Solutions

The following data is based on the product molecular weight 381.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.62 mL 13.11 mL 26.23 mL
5 mM 0.52 mL 2.62 mL 5.25 mL
10 mM 0.26 mL 1.31 mL 2.62 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Raeburn et al (1994) Anti-inflammatory and bronchodilator properties of RP 73401, a novel and selective phosphodiesterase type IV inhibitor. Br.J.Pharmacol. 113 1423 PMID: 7889300

Hatzelmann and Schudt (2001) Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J.Pharmacol.Exp.Ther. 297 267 PMID: 11259554

Zhao et al (2003) Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram. J.Pharmacol.Exp.Ther. 305 565 PMID: 12704225


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Keywords: RP73401 phosphodiesterases pde4 potent selective inhibitors inhibits RP 73401 Phosphodiesterases

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Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

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Asthma

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Pathways for Piclamilast

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