| Identification | Back Directory | [Name]
LIRIMILAST | [CAS]
329306-27-6 | [Synonyms]
LIRIMILAST
BAY 19-8004
BAY 19-8004 - Lirimilast
Urea,[2-(2,4-dichlorobenzoyl)-6-[(methylsulfonyl)oxy]-3-benzofuranyl]-
UREA, N-[2-(2,4-DICHLOROBENZOYL)-6-[(METHYLSULFONYL)OXY]-3-BENZOFURANYL]-
METHANESULFONIC ACID 2-(2,4-DICHLORO-BENZOYL)-3-UREIDO-BENZOFURAN-6-YL ESTER | [Molecular Formula]
C17H12Cl2N2O6S | [MDL Number]
MFCD09837901 | [MOL File]
329306-27-6.mol | [Molecular Weight]
443.26 |
| Chemical Properties | Back Directory | [Boiling point ]
663.2±55.0 °C(Predicted) | [density ]
1.619±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
12.33±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [IC 50]
PDE4: 42 nM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1016/S1094-5539(03)00090-7
[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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BOC Sciences
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MedChemExpress
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www.medchemexpress.com |
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