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BI-0115

Names

[ CAS No. ]:
4929-23-1

[ Name ]:
BI-0115

[Synonym ]:
6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 9-chloro-5,11-dihydro-5-propyl-
9-Chloro-5-propyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others

[In Vitro]

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].

[References]

[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).

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
489.2±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H14ClN3O

[ Molecular Weight ]:
287.744

[ Flash Point ]:
249.7±28.7 °C

[ Exact Mass ]:
287.082550

[ LogP ]:
3.08

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.602

Related Compounds