盐酸橡酰胺 T39740

Product Introduction
Bioactivity


英文名: Acoramidis hydrochloride

描述: Acoramidis hydrochloride (Alxn2060 hydrochloride) 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 hydrochloride 可用于转体甲状腺素淀粉样变性的研究。

体外活性: 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 (IC 50 > 100 μM) and a number of cytochrome P450 isozymes (IC 50 > 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.

体内活性: Animal Model: Wistar rats [1] . Dosage: 50 mg/kg/d (Toxicity Analysis). Administration: Oral gavage, daily for 28 d. Result: Showed the plasma C max 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

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 58.5 mg/mL (177.9 mM)


关键字: Alxn2060 Hydrochloride | AG-10 Hydrochloride | AG10 Hydrochloride | AG 10 Hydrochloride | Acoramidis Hydrochloride

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途