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Biological Activity for Piclamilast
Piclamilast is a 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 for Piclamilast
Technical Data for Piclamilast
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Piclamilast
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Piclamilast
The following data is based on the product molecular weight 381.25. Batch specific molecular weights may vary from batch to batch due to the degree 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|
References for Piclamilast
References are publications that support the biological activity of the product.
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 roflum. 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
If you know of a relevant reference for Piclamilast, please let us know.
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Keywords: Piclamilast, Piclamilast supplier, RP73401, phosphodiesterases, pde4, potent, selective, inhibitors, inhibits, RP, 73401, Phosphodiesterases, 4525, Tocris Bioscience
1 Citation for Piclamilast
Citations are publications that use Tocris products. Selected citations for Piclamilast include:
Zhang et al (2019) PDE1 inhibition facilitates proteasomal degradation of misfolded proteins and protects against cardiac proteinopathy. Sci Adv 5 eaaw5870 PMID: 31131329
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Literature in this Area
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