Piclamilast

Name: Piclamilast
Brand: Tocris Bioscience
SKU: 4525

Tocris Bioscience, part of Bio-Techne | Catalog # 4525

Citations (4)

COA / SDS

Potent and selective PDE4 inhibitor

Key Product Details

Description:	Potent and selective PDE4 inhibitor
Alternative Names:	RP 73401
Chemical Name:	3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide
Purity:	≥98% (HPLC)
Molecular Weight:	381.25

View Full Technical Details for Piclamilast

Technical Data
Citations

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	≥98% (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 for Piclamilast

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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.

Hatzelmann and Schudt Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflum. in vitro. J.Pharmacol.Exp.Ther. 2001 PMID: 11259554
Zhao Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [³H]piclamilast and [³H]rolipram. J.Pharmacol.Exp.Ther. 2003 PMID: 12704225
Raeburn Anti-inflammatory and bronchodilator properties of RP 73401, a novel and selective phosphodiesterase type IV inhibitor. Br.J.Pharmacol. 1994 PMID: 7889300