TES-991-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETES-991Cat. No.: HY-112619CAS No.: 1883602-20-7分式: CHNOS分量: 393.45作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 62.5 mg/mL (158.85 mM; Need ultrasonic)H2O : 40% PEG3

2、00 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.29 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.29 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 TES-991种有效的、有选择性的 -氨-羧粘康酸-半醛脱羧酶(ACMSD) 抑制剂，IC50 为3nM。IC50 & Target IC50:

3、 3 nM (hACMSD) 1.体外研究 TES-991 (compounds 21) is able to significantly increase intracellular NAD+ levels, providing further proof oftheir mechanism of action. TES-991 shows an inhibition of cytochrome P450 2C19, suggesting a possibleinvolvement of the 2H-tetrazole motif in this interaction 1.体内研究 Af

4、ter the intravenous administration of 0.5 mg/kg, TES-991 (compound 21) shows low blood clearance, withlow volumes of distribution and halflives (t1/2) of about 4.0 and 5.0 h, respectively, although after oraladministration at 5 mg/kg, the blood concentrations of TES-991 is quantifiable for up to 8 h

5、. A moderatesystemic exposure is observed for the 2H-tetrazole analogue, TES-991, a good systemic exposure isrecorded for the free acid 1.REFERENCES1. Pellicciari R, et al. -Amino-carboxymuconate-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De NovoNicotinamide Adenine Dinucleotide (NAD+) Biosynthesis. J Med Chem. 2018 Feb 8;61(3):745-759.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;