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 (1)
Reviews
Literature (2)

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

Piclamilast is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Piclamilast

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Piclamilast

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

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.

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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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


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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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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