| 产品描述： | Danuglipron (PF-06882961) 是一种非肽激动剂，仅在具有Trp33ECD的 Glucagon-like peptide-1 (GLP-1) receptor 中激活 canonical G protein 信号传导活性 |
| 靶点： |
GLP-1 receptor;GlucagonReceptor |
| 体外研究： |
PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R |
| 体内研究： |
PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys |
| 细胞实验： |
Cell lines: HEK293 cells Concentrations: 1 μM Incubation Time: 30 minutes Method: HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA |
| 动物实验： |
Animal Models: male cynomolgus monkeys Dosages: 1 mg/kg, 5 mg/kg, 100 mg/kg Administration: IV, Oral gavage |
| 参考文献： |
1. Hun Jee Choe, Young Min Cho. Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists. Endocrinol Metab (Seoul). 2021 Feb;36(1):22-29. 2. Griffith DA, et al. A small-molecule oral agonist of the human glucagon-like peptide-1 receptor. bioRxiv. 2020 Sep 30. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.8 ml |
8.999 ml |
17.999 ml |
| 5 mM |
0.36 ml |
1.8 ml |
3.6 ml |
| 10 mM |
0.18 ml |
0.9 ml |
1.8 ml |
| 50 mM |
0.036 ml |
0.18 ml |
0.36 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京