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TES-991
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TES-991图片
CAS NO:1883602-20-7
规格:98%
分子量:393.45
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TES-991是一种有效的、有选择性的人α-氨基-β-羧基粘康酸-ε-半醛脱羧酶(ACMSD)抑制剂,IC50为3nM。
CAS:1883602-20-7
分子式:C17H11N7OS2
分子量:393.45
纯度:98%
存储:Store at -20°C

Background:

TES-991 is a potent and selective human α?Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.


TES-991 (compounds 21) is able to significantly increase intracellular NAD+ levels, providing further proof of their mechanism of action. TES-991 shows an inhibition of cytochrome P450 2C19, suggesting a possible involvement of the 2H-tetrazole motif in this interaction[1].


After the intravenous administration of 0.5 mg/kg, TES-991 (compound 21) shows low blood clearance, with low volumes of distribution and halflives (t1/2) of about 4.0 and 5.0 h, respectively, although after oral administration at 5 mg/kg, the blood concentrations of TES-991 is quantifiable for up to 8 h. A moderate systemic exposure is observed for the 2H-tetrazole analogue, TES-991, a good systemic exposure is recorded for the free acid[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.