BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inter-ligand interactions at the receptor interfaces are key to the formation of the receptor tetramer thereby blocking oxLDL binding.
BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inter-ligand interactions at the receptor interfaces are key to the formation of the receptor tetramer thereby blocking oxLDL binding.
体外研究
BI-0115 can effectively reduce the internalization of oxLDL in cells. The IC50 value (5.4 μM) of cell experiments showed good consistency with the Kd values in SPR (4.3 μM) and ITC (6.99 μM) [1].
分子式
C15H14ClN3O
分子量
287.74
CAS号
4929-23-1
中文名称
BI-0115
运输条件
Room temperature in continental US; may vary elsewhere.