Comparison of Inhibitor and Substrate Selectivity between Rodent and Human Vascular Adhesion Protein-1

Table 1

Summary of inhibition in recombinant VAP-1 from mice, rats, and humans. IC₅₀ values are the mean and standard deviation of three separate determinations by nonlinear fit at varying concentrations in triplicate. Significance between mice and rats is indicated by ŧ. Significance between humans and mice is indicated by @. Significance between humans and rodents is indicated by .

Compound name	Chemical structure	IC50 (μM)
		Determined as described in Materials and Methods			Previously reported
		Mouse	Rat	Human	Mouse	Rat	Human
Semiarid (SEM)				^@	NR	NR	NR
Hydralazine (HYD)		^ŧ			NR	0.025; [31]	6.4; 26.5; [32]
LJP-1207					NR	0.0075; [22]	0.017; [22]
Astellas compound 35c					NR	0.072; [19]	0.02; [19]
PXS-4728A					0.021; [25]	0.018; [25]	0.005; [25]

^ŧ mouse vs. rat; human vs. mouse and rat; ^@ human vs. mouse. NR: not reported.