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Acoramidis hydrochloride
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 hydrochloride图片
CAS NO:2242751-53-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Alxn2060 hydrochloride
AG10 hydrochloride
产品介绍
Acoramidis 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。

产品描述

Acoramidis hydrochloride is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin) . Acoramidis hydrochloride is used in the study for transthyretin amyloidosis.

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

Cas No.

2242751-53-5

分子式

C15H18ClFN2O3

分子量

328.77

别名

Alxn2060 hydrochloride;AG10 hydrochloride;Acoramidis hydrochloride

储存和溶解度

DMSO:58.5mg/mL (177.9mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years