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Acoramidis
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Acoramidis图片
CAS NO:1446711-81-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AG10
产品介绍
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.
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
Clinical Trial
分子量

292.31

Formula

C15H17FN2O3

CAS 号

1446711-81-4

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.