4929-23-1

4929-23-1 structure

Name: BI-0115
Chemical Name: 9-Chloro-5-propyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
CAS Number: 4929-23-1
Molecular Formula: C₁₅H₁₄ClN₃O
Molecular Weight: 287.744
Catalog: Research Areas Cardiovascular Disease
Create Date: 2022-03-28 06:15:04
Modify Date: 2024-01-16 08:57:17
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].

Name	9-Chloro-5-propyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Synonyms	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

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).