Lirimilast

Modify Date: 2025-08-26 18:58:53

Lirimilast Structure
Lirimilast structure
Common Name Lirimilast
CAS Number 329306-27-6 Molecular Weight 443.25800
Density 1.619g/cm3 Boiling Point 663.2ºC at 760 mmHg
Molecular Formula C17H12Cl2N2O6S Melting Point N/A
MSDS N/A Flash Point 354.9ºC

 Use of Lirimilast


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].

 Names

Name [3-(carbamoylamino)-2-(2,4-dichlorobenzoyl)-1-benzofuran-6-yl] methanesulfonate
Synonym More Synonyms

 Lirimilast 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
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
InChIKey YPFLFUJKZDAXRA-UHFFFAOYSA-N
SMILES CS(=O)(=O)Oc1ccc2c(NC(N)=O)c(C(=O)c3ccc(Cl)cc3Cl)oc2c1

 Synonyms

Lirimilast
pumafentrine
UNII-GDK3KY5FCU
BAY-19-8004
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