TES-1025是一种有效的和选择性人α-氨基-β-羧基粘康酸-ε-半醛脱羧酶(ACMSD)抑制剂，IC50为13±3nM。
CAS：1883602-21-8
分子式：C18H13N3O3S2
分子量：383.44
纯度：98%
存储：Store at -20°C

Background:

TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13±3 nM.

TES-1025 is a low nanomolar human ACMSD inhibitor, which increases NAD+ levels in cellular systems[1].

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 (t1/2) 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 Cmax 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 AUC0-8h of 19?200 h?ng/mL and 36?600 h?ng/mL, respectively[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.