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Lirimilast

Catalog No. T15766   CAS 329306-27-6
Synonyms: BAY 19-8004

Lirimilast is an effective, selective, and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 49 nM). Lirimilast has potently anti-inflammatory properties. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease.

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Lirimilast Chemical Structure
Lirimilast, CAS 329306-27-6
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lirimilast is an effective, selective, and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 49 nM). Lirimilast has potently anti-inflammatory properties. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease.
Targets&IC50 PDE4:42 nM
In vitro Lirimilast is reported to be 5-fold more effective than Cilomilast and equipotent with CDP-840, In PDE4 assays, using freshly prepared PDE4 from human PMNL[1].
In vivo When compared in a rat model of lung neutrophilic inflammation, Lirimilast is found to be 3-fold more potent than Cilomilast. Since Lirimilast is orally active in the guinea-pig at 3 mg/kg and in primates at 0.1 mg/kg/day it appears to have a good therapeutic ratio [2].
Synonyms BAY 19-8004
Molecular Weight 443.26
Formula C17H12Cl2N2O6S
CAS No. 329306-27-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

Lirimilast 329306-27-6 Metabolism PDE BAY 19-8004 inhibitor inhibit

 

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