| 产品描述: | MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. |
| 靶点: |
IC50: 6.6 nM (glucagon receptor) |
| 体内研究: |
MK 0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowers ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduces glucose (AUC 0-6 h) by 32% and 39% at 3 and 10 mpk single doses, respectively. In hGCGR mice on a high fat diet, MK 0893 at 3, and 10 mpk po in feed lowers blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice |
| 参考文献: |
1. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.699 ml |
8.496 ml |
16.993 ml |
| 5 mM |
0.34 ml |
1.699 ml |
3.399 ml |
| 10 mM |
0.17 ml |
0.85 ml |
1.699 ml |
| 50 mM |
0.034 ml |
0.17 ml |
0.34 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |