TES-991

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

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

IC50: 3 nM (hACMSD)[1].

TES-991 (compounds 21) is able to significantly increase intracellular NAD+ levels, providing further proof of their mechanism of action. TES-991 shows an inhibition of cytochrome P450 2C19, suggesting a possible involvement of the 2H-tetrazole motif in this interaction[1].

After the intravenous administration of 0.5 mg/kg, TES-991 (compound 21) 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[1].

[1]. Pellicciari R, et al. α-Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De Novo Nicotinamide Adenine Dinucleotide (NAD+) Biosynthesis. J Med Chem. 2018 Feb 8;61(3):745-759.

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