Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC 50 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PDE4 42 nM (IC 50 )
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Lirimilast
CAS number:329306-27-6 molecular formula:C17H12Cl2N2O6S
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| Chinese alias | 利美司特 | 2-(2,4-二氯苯甲酰基)-3-脲基苯并呋喃-6-基甲磺酸酯 | ||
| English alias | LIRIMILAST [WHO-DD] | NCGC00263118-01 | BAY19-8004 | Q27279046 | E98791 | MS-27976 | Cefaclor-1-wasser | EINECS 274-322-7 | Lirimilast | 2-(2,4-Dichlorobenzoyl)-3-ureidobenzofuran-6-yl methanesulfonate | SMR004703312 | SR-01000945274-1 | EX-A5382 | SR-010 | ||
| CAS number | 329306-27-6 | molecular formula | C17H12Cl2N2O6S |
| molecular weight | 443.26 g/mol | Exact mass | - |
| PSA | 137.000 Ų | logp | 4 |
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