| Bioactivity | TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM[1]. | ||||||||||||
| Target | IC50: 13±3 nM (human ACMSD) | ||||||||||||
| Invitro | 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 (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]. | ||||||||||||
| Name | TES-1025 | ||||||||||||
| CAS | 1883602-21-8 | ||||||||||||
| Formula | C18H13N3O3S2 | ||||||||||||
| Molar Mass | 383.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |