AG-10

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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).Western Blot Analysis.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.

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

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Other Targets

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1446711-81-4

292.31

C15H17FN2O3

>98% (HPLC)

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O(CCCC=1C(C)=NNC1C)C2=CC(C(O)=O)=CC=C2F

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(-20℃)

With Ice Pack

≥ 2 years