TES-1025

目录号: PL08489 纯度: ≥98%
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 nM。
CAS No. :1883602-21-8
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中文名称
TES-1025
中文别名
化合物 T17042;化合物TES-1025
英文名称
TES-1025
英文别名
TES-1025;2-(3-(((5-cyano-6-oxo-4-(thiophen-2-yl)-1,6-dihydropyrimidin-2-yl)thio)methyl)phenyl)acetic acid;Benzeneacetic acid, 3-[[[5-cyano-1,6-dihydro-6-oxo-4-(2-thienyl)-2-pyrimidinyl]thio]methyl]-;inhibit,Inhibitor,TES 1025,TES1025,TES-1025
Cas No.
1883602-21-8
分子式
C18H13N3O3S2
分子量
383.44
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
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 nM。
产品详情
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 nM。
生物活性
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC 50 of 13 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 13±3 nM (human ACMSD)
体外研究(In Vitro)
TES-1025 is a low nanomolar human ACMSD inhibitor, which increases NAD levels in cellular systems. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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 (t 1/2 ) 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 C max 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 AUC 0-8h of 19?200 h?ng/mL and 36?600 h?ng/mL, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (260.80 mM; Need warming)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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