AR-125(AR-125) - 在研适应症：自身免疫性肝炎_专利_临床

概要

基本信息

药物类型

未知

别名

靶点-

作用方式-

作用机制-

治疗领域

免疫系统疾病消化系统疾病

在研适应症

自身免疫性肝炎

非在研适应症-

原研机构

吉亚生物科技有限公司

在研机构

吉亚生物科技有限公司

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 AR-125 相关的临床结果

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100 项与 AR-125 相关的转化医学

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100 项与 AR-125 相关的专利（医药）

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1

项与 AR-125 相关的文献（医药）

2012-01-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Virtual ligand screening of α-glucosidase: Identification of a novel potent noncarbohydrate mimetic inhibitor

4区 · 医学

Article

作者: Takumi Tsukagoshi ; Ryosuke Ishikawa ; Wataru Hakamata ; Toshiyuki Nishio ; Takako Hirano ; Saori Tamura ; Yoriko Ushijima

5-Thiazoleacetamide derivatives of AR122 and AR125 were screened as α-glucosidase inhibitors by in silico high-throughput screening from commercial drug-like small compound libraries. Inhibition of α-glucosidase with AR122 and AR125 is time dependent: with no preincubation, AR122 and AR125 are relatively moderate inhibitors, but interestingly, after a 120 min incubation, they were 50-fold more potent (AR122: IC(50)=2.47 μM and AR125: IC(50)=27.1 μM). Plots of ln [residual α-glucosidase activity %] versus preincubation time show a pseudo-first order kinetics for both inhibitors. Through dialysis of enzyme-inhibitor complexes, no activity recovery was shown. These results suggest that AR122 and AR125 constitute a new class of noncarbohydrate mimetic inhibitor with an irreversible mechanism.

100 项与 AR-125 相关的药物交易

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