Lirimilast (BAY 19-8004) 是一种有效的，选择性的和口服活性的磷酸二酯酶 4 (PDE4) 抑制剂，IC50 值为 49 nM。Lirimilast 可用于哮喘或慢性阻塞性肺疾病 (COPD) 的研究，具有强效的抗炎特性。
| 生物活性 |
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. |
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| 体外研究 |
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. |
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| 体内研究 |
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.
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| 分子式 |
C17H12N2O6Scl2
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| 分子量 |
443.26
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| CAS号 |
329306-27-6
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： ≥98%
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