化合物BF738735
中文名称 | 化合物BF738735 |
---|---|
中文同义词 | 2-氟-4-(2-甲基-8-((3-(甲基磺酰基)苄基)氨基)咪唑并[1,2-A]吡嗪-3-基)苯酚;化合物 T16530;化合物BF738735;2-氟-4-[2-甲基-8-[[3-(甲砜基)苄基]氨基]-3-咪唑并[1,2-A]吡嗪基]苯酚 |
英文名称 | 2-fluoro-4-(2-methyl-8-((3-(methylsulfonyl)benzyl)amino)imidazo[1,2-a]pyrazin-3-yl)phenol |
英文同义词 | 2-fluoro-4-(2-methyl-8-((3-(methylsulfonyl)benzyl)amino)imidazo[1,2-a]pyrazin-3-yl)phenol;BF738735;BF738735 (BF 738735;Phenol, 2-fluoro-4-[2-methyl-8-[[[3-(methylsulfonyl)phenyl]methyl]amino]imidazo[1,2-a]pyrazin-3-yl]-;BF738735,Phosphatidylinositol 4 kinases,Inhibitor,BF 738735,PI4 kinases,inhibit,BF-738735,Reverse Transcriptase,PI4K;2-Fluoro-4-[2-methyl-8-[[3-(methylsulfonyl)benzyl]amino]-3-imidazo[1,2-a]pyrazinyl]phenol |
CAS号 | 1436383-95-7 |
分子式 | C21H19FN4O3S |
分子量 | 426.46 |
EINECS号 | |
相关类别 | |
Mol文件 | 1436383-95-7.mol |
结构式 | ![]() |
化合物BF738735 性质
密度 | 1.42±0.1 g/cm3(Predicted) |
---|---|
储存条件 | Store at -20°C |
溶解度 | 二甲基亚砜:125 mg/ml(293.11 mM) |
酸度系数(pKa) | 8.08±0.20(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
PI4KIIIβ 5.7 nM (IC 50 ) |
PI4KIIIα 1.7 μM (IC 50 ) |
BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC 50 of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC 50 of 1.7 μM). In addition, the activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 potently inhibits all viruses tested, with EC 50 s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC 50 and using the same culture conditions for 3 to 4 days, is low, with CC 50 values ranging from 11 to 65 μM, resulting in high selectivity indices. Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC 50 of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3).
BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-U00426 | BF738735 | 1 mg | 419元 | |
2024/04/30 | HY-U00426 | 暂无 BF738735 | 1436383-95-7 | 10mM * 1mLin DMSO | 1320元 |