化合物BI 1015550 T72031

Product Introduction
Bioactivity


英文名: BI 1015550

描述: BI 1015550 是一种具有口服活性的PDE4B 抑制剂，IC50值为 7.2 nM。BI 1015550 具有良好的安全性，在炎症、过敏疾病、肺纤维化和慢性阻塞性肺疾病 (COPD) 中有潜在应用。

体外活性: BI 1015550 inhibited Lipopolysaccharides-induced TNF-α release and Phytohemagglutinin P-induced IL-2 release in human PBMCs with IC50 values of 35 nM and 9 nM, respectively.[2 BI 1015550 inhibited the release of TNF-α in rat whole blood with an IC50 value of 91 nM.[2]

体内活性: BI 1015550 (Example 2) (0, 0.3, 1.0 and 3.0 mg/kg ; oral ; single dose) at 1.0 mg/kg weakened intestinal transit in rats, but did not significantly affect body weight.[1] BI 1015550 prevented inflammation in rat lung tissue with an ED50 value of 0.1 mg/kg.[1] BI 1015550 (0.01, 0.1 and 1.0 mg/kg ; oral ; single dose) reduced Lipopolysaccharides-induced TNF-α release in mouse plasma in a dose-dependent manner.[2] BI 1015550 (0.1, 0.3 and 1.0 mg/kg ; oral ; single dose) inhibited lipopolysaccharide-induced neutrophil entry into the bronchoalveolar lavage fluid of male Suncus Murinus and Wistar rats.[2] BI 1015550 (2.5 mg/kg and 12.5 mg/kg ; oral ; twice a day for 6 days) was effective in ameliorating the damage caused by bleomycin in mice.[2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.49 mg/mL (10 mM)


关键字: BI 1015550 | BI1015550 | BI-1015550

相关产品: Tanimilast | Enpp/Carbonic anhydrase-IN-1 | PF-00489791 | FPFT-2216 | WAY-313170 | Autotaxin-IN-5 | AMG 579 | MR-L2 | Z-HA155 | Roflumilast

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途