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AG-10 (Acoramidis) 是选择性的、口服有效的甲状腺素转运蛋白 (TTR (transthyretin)) 的稳定剂,显示出对野生型和 V1221 突变型均有效。
AG-10 (Acoramidis) 是选择性的、口服有效的甲状腺素转运蛋白 (TTR (transthyretin)) 的稳定剂,显示出对野生型和 V1221 突变型均有效。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,080 | 现货 | |
5 mg | ¥ 2,390 | 现货 | |
10 mg | ¥ 3,590 | 现货 | |
25 mg | ¥ 5,750 | 现货 | |
50 mg | ¥ 7,770 | 现货 | |
100 mg | ¥ 9,870 | 现货 | |
200 mg | ¥ 13,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,180 | 现货 |
产品描述 | AG-10 (Acoramidis) 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. |
体外活性 | 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]. |
体内活性 | 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]. |
别名 | Acoramidis |
分子量 | 292.31 |
分子式 | C15H17FN2O3 |
CAS No. | 1446711-81-4 |
Smiles | O(CCCC=1C(C)=NNC1C)C2=CC(C(O)=O)=CC=C2F |
密度 | 1.282 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 4.8 mg/mL (16.42 mM) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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