BI-0115 是 LOX-1 的选择性抑制剂(IC50=5.4 µM)，阻止细胞摄取氧化低密度脂蛋白。BI-0115 结合通过形成同二聚体配体结合域的二聚体触发受体抑制。
货号:ajcx36774
CAS:4929-23-1
分子式:C15H14ClN3O
分子量：287.74
溶解度:DMSO : 100 mg/mL (347.54 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain[1].

BI-0115 efficiently reduces oxLDL internalization in the cellular context. The IC50 values of the cellular assay (5.4 µM) are in good agreement with the determined Kd values in SPR (4.3 µM) and ITC (6.99 µM)[1].

[1]. Schnapp, G., et al. A small-molecule inhibitor of lectin-like oxidized LDL receptor-1 acts by stabilizing an inactive receptor tetramer state. Commun Chem 3, 75 (2020).