Introduction：Basic information about CAS 329306-27-6|Lirimilast, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Lirimilast |
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| CAS Number | 329306-27-6 | Molecular Weight | 443.25800 |
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| Density | 1.619g/cm3 | Boiling Point | 663.2ºC at 760 mmHg |
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| Molecular Formula | C17H12Cl2N2O6S | Melting Point | / |
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| MSDS | / | Flash Point | 354.9ºC |
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Names
| Name | [3-(carbamoylamino)-2-(2,4-dichlorobenzoyl)-1-benzofuran-6-yl] methanesulfonate |
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| Synonym | More Synonyms |
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Lirimilast BiologicalActivity
| 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]. |
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| Related Catalog | Signaling Pathways >>Metabolic Enzyme/Protease >>Phosphodiesterase (PDE)Research Areas >>Inflammation/Immunology |
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| Target | PDE4:42 nM (IC50) |
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| 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]. |
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| 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]. |
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| 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. |
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Chemical & Physical Properties
| Density | 1.619g/cm3 |
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| Boiling Point | 663.2ºC at 760 mmHg |
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| Molecular Formula | C17H12Cl2N2O6S |
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| Molecular Weight | 443.25800 |
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| Flash Point | 354.9ºC |
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| Exact Mass | 441.97900 |
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| PSA | 138.07000 |
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| LogP | 5.46720 |
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| Index of Refraction | 1.677 |
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| InChIKey | YPFLFUJKZDAXRA-UHFFFAOYSA-N |
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| SMILES | CS(=O)(=O)Oc1ccc2c(NC(N)=O)c(C(=O)c3ccc(Cl)cc3Cl)oc2c1 |
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Synonyms
| Lirimilast |
| pumafentrine |
| UNII-GDK3KY5FCU |
| BAY-19-8004 |
