TES-991 is a potent and selective inhibitor of human α Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD)(IC50 of 3 nM).

ACMSD (human):3 nM

TES-991 significantly increase intracellular NAD+ levels, providing further proof of their mechanism of action. TES-991 exhibits an inhibition of cytochrome P450 2C19, suggesting a possible involvement of the 2H-tetrazole motif.

TES-991(intravenous,0.5 mg/kg) shows low blood clearance, with low volumes of distribution and halflives (t1/2) of about 4.0 and 5.0 h, respectively, although after oral administration at 5 mg/kg, the blood concentrations of TES-991 is quantifiable for up to 8 h. A moderate systemic exposure is observed for the 2H-tetrazole analogue, TES-991, a good systemic exposure is recorded for the free acid.