TES-1025

TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC₅₀ of 13 nM^[1]. IC50 & Target: IC50: 13±3 nM (human ACMSD)^[1] In Vitro: TES-1025 is a low nanomolar human ACMSD inhibitor, which increases NAD⁺ levels in cellular systems^[1]. In Vivo: TES-1025 is subjected to in vivo pharmacokinetic studies, following intravenous (IV) and oral (PO) dosings of male CD-1 mice. After the intravenous administration of 0.5 mg/kg, TES-1025 shows low blood clearance, with low volumes of distribution and half-lives (t_1/2) of about 5.33 h, although after oral administration at 5 mg/kg, the blood concentration of TES-1025 is quantifiable for up to 8 h. A good systemic exposure is recorded for TES-1025, with a C_max of 2570 ng/mL reaches at 2 h after dosing. The greater oral exposure of TES-1025 is further confirmed in the liver and kidneys with AUC_0-8h of 19?200 h?ng/mL and 36?600 h?ng/mL, respectively^[1].