LYS006 is a highly efficient and selective LTA4H (leukotriene A4 hydrolase) inhibitor, which can be used for neutrophil-driven inflammatory diseases such as ulcerative colitis.

Method:
In vitro assays were conducted to evaluate the inhibitory effect of LYS006 on LTA4H enzymatic activity using Arg-AMC (arginine conjugated with 7-amino-4-methylcoumarin) as the substrate, with an incubation time of 15 minutes. Additionally, a human whole blood (hWB) assay was performed with a 30-minute treatment to assess the inhibition of LTB4 biosynthesis.

Result:
LYS006 effectively inhibited the hydrolysis of Arg-AMC catalyzed by LTA4H within 15 minutes, with an IC₅₀ of 2 nM. In the hWB assay, 30-minute treatment with LYS006 inhibited LTB4 biosynthesis, with an IC₅₀ of 167 nM. [1]

Method:
Mice were administered a single oral dose of LYS006 (0.3 mg/kg), and the inhibition of LTB4 release was evaluated in comparison to the vehicle control group.
Result:
LYS006 inhibited approximately 43% of LTB4 release compared to the vehicle control group. [1]