329306-27-6
中文名称
LIRIMILAST
英文名称
LIRIMILAST
CAS
329306-27-6
分子式
C17H12Cl2N2O6S
分子量
443.26
MOL 文件
329306-27-6.mol
329306-27-6 结构式
基本信息
中文别名
化合物 T15766 英文别名
LIRIMILASTBAY 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
物理化学性质
沸点663.2±55.0 °C(Predicted)
密度1.619±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)12.33±0.30(Predicted)
形态Solid
颜色White to off-white
常见问题列表
生物活性
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。靶点
|
PDE4 42 nM (IC 50 ) |
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.
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.