AMG-3969
| 中文名称 | AMG-3969 |
|---|---|
| 中文同义词 | 4-[(2S)-4-[(6-氨基-3-吡啶基)磺酰基]-2-(1-丙炔-1-基)-1-哌嗪基]-Α,Α-双(三氟甲基)-苯甲醇;AMG-3969游离态;化合物AMG-3969;(S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 |
| 英文名称 | AMG-3969 |
| 英文同义词 | AMG-3969;CS-2503;AMG-3969; AMG 3969; AMG3969;Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)-;Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)-;(S)-2-(4-(4-((6-Aminopyridin-3-yl)sulfonyl)-2-(prop-1-yn-1-yl)piperazin-1-yl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol;Hexokinase IV,AMG 3969,Hexokinase D,Glucokinase,Inhibitor,AMG3969,AMG-3969,inhibit;2-[4-[(2S)-4-[(6-amino-3-pyridyl)sulfonyl]-2-prop-1-ynyl-piperazin-1-yl]phenyl]-1,1,1,3,3,3-hexafluoro-propan-2-ol |
| CAS号 | 1361224-53-4 |
| 分子式 | C21H20F6N4O3S |
| 分子量 | 522.46 |
| EINECS号 | |
| 相关类别 | 有机化学 |
| Mol文件 | 1361224-53-4.mol |
| 结构式 |  |
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) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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.
安全信息
| 海关编码 | 2935909099 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12411 | AMG-3969 AMG-3969 | 1361224-53-4 | 1mg | 1200元 |
| 2024/04/30 | HY-12411 | AMG-3969 AMG-3969 | 1361224-53-4 | 5mg | 2800元 |