MF-152(MF-152) - 药物靶点：SCD1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

MF-152

靶点

SCD1

作用方式

抑制剂

作用机制

SCD1抑制剂(酰基辅酶A去饱和酶抑制剂)

治疗领域

内分泌与代谢疾病

在研适应症-

非在研适应症

代谢性疾病

原研机构

Merck Canada, Inc.

在研机构-

非在研机构

Merck Canada, Inc.

权益机构-

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 MF-152 相关的临床结果

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100 项与 MF-152 相关的转化医学

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100 项与 MF-152 相关的专利（医药）

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2

项与 MF-152 相关的文献（医药）

2011-10-01·Bioorganic & medicinal chemistry letters4区 · 医学

Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: From systemic to liver-targeting inhibitors

4区 · 医学

Article

作者: Black, Cameron ; Isabel, Elise ; Ramtohul, Yeeman K. ; Huang, Zheng ; Powell, David ; Zhang, Lei ; Guay, Jocelyne ; Robichaud, Joel ; Leger, Serge ; Li, Chun Sing ; Leclerc, Jean-Philippe ; Crane, Sheldon ; Oballa, Renata ; Guiral, Sebastien

Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eyes where adverse effects were previously observed in rodents, representative systemically-distributed SCD1 inhibitors were converted into liver-targeting SCD1 inhibitors.

2010-03-01·Bioorganic & medicinal chemistry letters4区 · 医学

SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors

4区 · 医学

Article

作者: Zhang, Lei ; Li, Chun Sing ; Ramtohul, Yeeman K. ; Black, Cameron ; Guay, Jocelyne ; Huang, Zheng ; Chan, Chi-Chung ; Xu, Li-Jing ; Guiral, Sebastien ; Crane, Sheldon ; Oballa, Renata

Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC(50)=1nM) was identified from the optimization of a lead thiazole compound MF-152 with over 100-fold improvement in potency. In a 4-week chronic oral dosing at 0.2mg/kg, 3j gave a robust 24% prevention of body weight gain in mice fed on a high fat diet accompanied with an improved metabolic profile on insulin and glucose levels.

100 项与 MF-152 相关的药物交易

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