AcumaPimod 是一种有口服活性的p38 MAP激酶抑制剂,IC50值小于1 μM。
产品描述
Acumapimod is an orally active inhibitor of p38α MAPK (IC50<1 μM).
体内活性
Acumapimod increases survival and reduces the number of macrophages in bronchoalveolar lavage fluid (BALF) in a mouse model of infection with influenza H1N1 A/PR/8/34 when administered at a dose of 6 mg/kg[1]
动物实验
In vivo, female BALB/c mice were infected intranasally with 150 pfu of influenza H1N1 A/Puerto Rico/8/34 and treated with Acumapimod(BCT197) (a closely related p38 MAPK inhibitor with an IC50 value of<1?μM, currently in clinical testing), dexamethasone or oseltamivir (Tamiflu) starting 24?h post infection. Body weight, bronchoalveolar lavage cells, cytokines, total protein and lactate dehydrogenase as well as serum cytokines were measured; a subset of animals was evaluated histopathologically[1].
Cas No.
836683-15-9
分子式
C22H19N5O2
分子量
385.427
别名
BCT-197
储存和溶解度
DMSO:50 mg/mL (129.73 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years