Lirimilast

Names

[ Name ]:
Lirimilast

[Synonym ]:
Lirimilast
pumafentrine
UNII-GDK3KY5FCU
BAY-19-8004

Biological Activity

[Description]:

Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Inflammation/Immunology

[Target]

PDE4:42 nM (IC50)

[In Vitro]

In PDE4 assays Lirimilast (BAY 19-8004) is reported to be 5-fold more potent than Cilomilast and equipotent with CDP-840 using freshly prepared PDE4 from human PMNL[1].

[In Vivo]

Since Lirimilast (BAY 19-8004) is orally active in the guinea-pig at 3 mg/kg and, more critically, in primates at 0.1 mg/kg/day it appears to have a good therapeutic ratio. In addition Lirimilast is found to be 3-fold more potent than Cilomilast when compared in a rat model of lung neutrophilic inflammation[2].

[References]

[1]. Grootendorst DC, et al. Efficacy of the novel phosphodiesterase-4 inhibitor BAY 19-8004 on lung function and airway inflammation in asthma and chronic obstructive pulmonary disease (COPD). Pulm Pharmacol Ther. 2003;16(6):341-7.

[2]. Peter Norman. PDE4 inhibitors: sustained patenting activity as leading drugs near the market. Exp. Opin. Ther. Patents (2000) 10(9):1415-1427.

Chemical & Physical Properties

[ Density]:
1.619g/cm3

[ Boiling Point ]:
663.2ºC at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₂Cl₂N₂O₆S

[ Molecular Weight ]:
443.25800

[ Flash Point ]:
354.9ºC

[ Exact Mass ]:
441.97900

[ PSA ]:
138.07000

[ LogP ]:
5.46720

[ Index of Refraction ]:
1.677

Related Compounds

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