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.
| 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
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
Keywords: Piclamilast, supplier, RP73401, phosphodiesterases, pde4, potent, selective, inhibitors, inhibits, RP, 73401, Phosphodiesterases, Phosphodiesterases, Tocris Bioscience
