| 产品描述: | Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. |
| 体外研究: |
Lesogaberan hydrochloride potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve. Oral Lesogaberan (0.08 mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice. Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats. |
| 体内研究: |
Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro. |
| 参考文献: |
1. Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12. 2. Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539. |
| 保存条件: |
-80°C 6个月; -20°C 1个月,氮气保存,干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
5.633 ml |
28.163 ml |
56.325 ml |
| 5 mM |
1.127 ml |
5.633 ml |
11.265 ml |
| 10 mM |
0.563 ml |
2.816 ml |
5.633 ml |
| 50 mM |
0.113 ml |
0.563 ml |
1.127 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。 |