Acoramidis (AG10) 是具有口服活性的、选择性的甲状腺素转运蛋白 (TTR (transthyretin)) 的稳定剂，对野生型和 V1221 突变型均有效。Acoramidis (AG10) 可用于转体甲状腺素淀粉样变性的研究。
| 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 fortransthyretinamyloidosis[1][2]. |
体外研究
(In Vitro) | 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[1].
Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM[3].
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)[1].
Western Blot Analysis[1]. | Cell Line: | Human serum (TTR ~5 μM). | | Concentration: | 0.1 and 10 μM. | | Incubation Time: | 72 h. | | Result: | Was significantly more effective than tafamidis in stabilizing TTR.
The concentration of AG10 to 10 μM resulted in stabilization of almost all of TTR in serum. |
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体内研究
(In Vivo) | | Animal Model: | Wistar rats[1]. | | Dosage: | 50 mg/kg/d (Toxicity Analysis). | | Administration: | Oral gavage, daily for 28 d. | | Result: | Showed the plasma Cmaxof ~40 μM and histopathological evaluation of liver, kidney, heart, spleen, thymus, and lung showed no signs of pathologic processes in the AG10-treated animals |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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