AMG-3969

    • 货号:MC1367
      • CasNo:
      • 1361224-53-4
      • 分子式:
      • C21H20F6N4O3S
      • 纯度:
      • >98%
      • 靶点:
      • Glucokinase
      • IC50:
      • IC50: 4 nM (GK-GKRP)[1]
      • 体外研究:
      • AMG-3969 exhibits potent cellular activity with an EC50 of 0.202 μM and IC50 of 4 nM[1], [2]. It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes)[3].
      • 体内研究:
      • AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice[1]. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point[2]. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/oband db/db mice; however,AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose[3].
      • 简介:
      • AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.
      • 特异性:
      • Target: Glucokinase. Fields: AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.
      • 稀释:
      • IC50: 4 nM (GK-GKRP)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • AMG3969,AMG 3969
      • 分子量:
      • 522.46
      • 产品图片