| Description | TES-991 is a potent and selective inhibitor of human α Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD)(IC50 of 3 nM). |
| In vitro | 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. |
| In vivo | 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. |
| Target activity | ACMSD (human):3 nM |
| molecular weight | 393.45 |
| Molecular formula | C17H11N7OS2 |
| CAS | 1883602-20-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 62.5 mg/mL (158.85 mM), Sonication is recommended. |
| References | 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. |