产品
编 号：F166061
分子式：C15H17FN2O3
分子量：292.31
分子式：C15H17FN2O3
分子量：292.31
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1446711-81-4
产品详情
生物活性：
Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis.
体内研究：
Animal Model:Wistar rats.
Dosage:50 mg/kg/d (Toxicity Analysis).
Administration:Oral gavage, daily for 28 d.
Result:Showed the plasma Cmax of ～40 μM and histopathological evaluation of liver, kidney, heart, spleen, thymus, and lung showed no signs of pathologic processes in the AG10-treated animals
体外研究：
Acoramidis (AG10, 0.1-10 μM for TTR ～5 μM) stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum.Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM.Acoramidis (AG10) has very 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).
Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis.
体内研究：
Animal Model:Wistar rats.
Dosage:50 mg/kg/d (Toxicity Analysis).
Administration:Oral gavage, daily for 28 d.
Result:Showed the plasma Cmax of ～40 μM and histopathological evaluation of liver, kidney, heart, spleen, thymus, and lung showed no signs of pathologic processes in the AG10-treated animals
体外研究：
Acoramidis (AG10, 0.1-10 μM for TTR ～5 μM) stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum.Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM.Acoramidis (AG10) has very 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).
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