Piclamilast

Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively[1][2][3][4].

Product Specifications

CAS Number

[144035-83-6]

Product Name Alternative

RP 73401; RPR 73401

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/piclamilast.html

Purity

99.74

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC)C(OC3CCCC3)=C2

Molecular Formula

C18H18Cl2N2O3

Molecular Weight

381.25

Precautions

H302, H315, H319, H335

References & Citations

[1]M J Ashton, et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3- (cyclopentyloxy) -4-methoxybenzamides and analogues. J Med Chem. 1994 May 27;37 (11) :1696-703.|[2]Manuel Mata, et al. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H (2) O (2) via mechanisms involving AP-1 activation. Free Radic Res. 2012 May;46 (5) :690-9.|[3]Edoardo Parrella, et al. Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways. J Biol Chem . 2004 Oct 1;279 (40) :42026-40.|[4]T Ukita, et al. Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. J Med Chem. 1999 Mar 25;42 (6) :1088-99.