AMG-3969
AMG-3969 性质
| 沸点 | 648.8±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.56±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | DMSO:100.0(最大浓度 mg/mL);191.4(最大浓度 mM) |
| 酸度系数(pKa) | 10.12±0.15(Predicted) |
AMG-3969 用途与合成方法
IC50: 4 nM (GK-GKRP)
AMG-3969 exhibits potent cellular activity with an EC 50 of 0.202 μM and IC 50 of 4 nM, . It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes).
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. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/ob and 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.
AMG-3969 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-12411 | AMG-3969 | 1361224-53-4 | 1mg | 1500 |
| 2024-01-25 | HY-12411 | AMG-3969 | 1361224-53-4 | 5mg | 3500 |
