產品屬性：
產品名稱 | Lesogaberan |
規格 | 5 mg、10 mg、25 mg、50 mg |
貨號 | EY-01Y14114 |
Cas No.: 344413-67-8
別名: N/A
化學名: N/A
分子式: C3H9FNO2P
分子量: 141.08
溶解度: N/A
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2]. Cell Proliferation Assay[2] Cell Line:Human islet cellsLesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1].Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2]. Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].
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