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产品介绍
产品介绍
产品信息
商品描述
AG-10 is an orally active and selective kinetic stabilizer of TTR (transthyretin). AG-10 exhibits activity for WT and V122I-TTR. AG-10 is used in the study of transthyretin amyloidosis.
分子量
292.31
纯度
98%
可溶性
DMSO:4.8 mg/mL (16.42 mM)
In vitro(体外研究)
AG-10 (0.1-10 μM for TTR ∼5 µM) stabilizes WT- and V122I-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum. AG-10 exhibits minimal inhibition of two common off-targets in drug discovery, the potassium ion channel hERG (IC50 > 100 µM) and a number of cytochrome P450 isozymes (IC50 > 50 µM) (low toxicity)[1]. AG-10 (10-100 μM) stimulates the mitochondrial QO2 in a concentration-dependent manner[2].
In vivo(体内研究)
AG-10 (Oral gavage; 50 mg/kg/d; daily for 28 d) exhibited the plasma Cmax of ∼40 µM and histopathological evaluation of liver, thymus, kidney, spleen, heart, and lung showed no signs of pathologic processes in the AG10-treated Wistar rats[1].
背景
分子式
C15H17FN2O3
CAS号
1446711-81-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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