BI-0115

Research use only, not for human use.

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.

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 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).

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Immunology/Inflammation

Lipoxygenase

LOX-1

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4929-23-1

287.747

C15H14ClN3O

>98% (HPLC)

DMSO:10 mM

O=C1N(CCC)C2=CC=CN=C2NC3=C1C=CC(Cl)=C3

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(-20℃)

With Ice Pack

≥ 2 years