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TES-1025-DataSheet-MedChemExpress

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Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Data Sheet Product Name: Cat. No.: CAS No.: Molecular Formula: Molecular Weight: Target: Pathway: Solubility: TES-1025 HY-111365 1883602-21-8 C18H13N3O 3S2 383.44 Others Others DMSO: 100 mg/mL (Need warming) BIOLOGICAL ACTIVITY:   TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD ) inhibitor with an IC50 of 13±3 nM. 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 istration of 0.5 mg/kg, TES-1025 shows low blood clearance, with low volumes of distribution and halflives (t1/2) of about 5.33 h, although after oral istration 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 1]. 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[   Kinase Assay: [1]Recombinant hACMSD is expressed in Pichia pastoris and purif. Its enzyme activity is assayed by a coupled PROTOCOL (Extracted from published papers and Only for reference) spectrophotometric assay. Briefly, in a pre-assay mixture, the ACMS substrate is generated from 10 μM 3-hydroxyanthranilic acid by recombinant 3-hydroxyanthranilate 3,4-dioxigenase from Ralstonia metallidurans. ACMS formation is monitored at 360 nm, and after the reaction is complete, an appropriate amount of ACMSD is added. Activity is calculated from the initial rate of the absorbance decrease subtracted from that of a control reaction mixture in the absence of ACMSD. The effects of the various compounds (e.g., TES-1025) on the enzyme activity are tested by adding the compounds to the assay mixture along with ACMSD. For the IC50 evaluatio ns for each compound, a serial dilution from a stock solution prepared in DMSO is tested, maintaining a DMSO concentration in all the reaction mixtures of 1.0%. One unit is defined as the amount of enzyme that consume 1 μmol of ACMS per minute at 37°C[1]. Animal istration: [1]Mice[1] Male CD-1 mice are used.The study is conducted in 3 phases. Phase 1: 18 mice receive an oral istration of TES-1025 at a target dose level of 5 mg/kg. Blood, brain and liver are collected at intervals up to 8 h after dose istration (n=3 animals per each time point). Phase 2: 3 mice receive each an intravenous istration of TES-1025 at a target dose of 0.5 mg/kg. Blood samples are collected from the lateral tail vein at intervals up to 24 h after dose istration. Phase 3: 3 mice receive a single intravenous istration of Elacridar (5 mg/kg) shortly before an oral istration of TES-1025 at a target dose of 5 mg/kg. Blood and brain samples are collected 0.5 h after dose istration. Brain, liver and kidney are collected from all animals of the study[1].   References: [1]. Pellicciari R, et al. α-Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De Novo Nicotinamide www.MedChemExpress.com

TES-1025-heet-MedChemExpress

Adenine Dinucleotide (NAD+) Biosynthesis. J Med Chem. 2018 Feb 8;61(3):745-759. Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898     Fax: 609-228-5909     E-mail: tech@MedChemExpress.com Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA www.MedChemExpress.com

TES-1025-heet-MedChemExpress

TES-1025-heet-MedChemExpress

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