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Lesogaberan  ≥98%

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包装规格：5mg in glass bottle
产品描述：基本信息 产品编号： L10500 产品名称： Lesogaberan CAS: 344413-67-8   储存条件 粉末 -20℃ 四年 分子式： C3H9FNO2P 溶于液体 -80℃ 二年 分子量： 141.08     化学名：  [(2R)-3-amino-2-fluoropropyl]-hydroxy-oxophosphanium Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种有效的选择性GABAB受体激动剂 靶点 Ki:5.1±1.2nM (rat GABAB),1.4±0.3μM (rat GABAA) EC50:8.6±0.77nM (human GABAB receptor) 体外研究 Lesogaberan (3-30nM) enhances human islet cell proliferation in vitro. Cell Proliferation Assay Cell Line: Human islet cells Concentration: 3,10,and 30nM Incubation Time: 4 days Result: Had a small but nonsignificant promitotic effect at 3nM,while treatment at higher dosages (10 and 30nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone. 体内研究 Lesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs,with a biphasic dose-response curve.Oral Lesogaberan (0.08mg/mL;48 hours) protects human islet β-cells from apoptosis in islet grafts in mice.Lesogaberan (7μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats. Animal Model: Diabetic NOD/scid mice were implanted with human islets Dosage: 0.08mg/mL Administration: Oral feeding;48 hours Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+β-cells in human islet grafts.   Animal Model: Female Sprague Dawley rats Dosage: 7μmol/kg (Pharmacokinetic Analysis) Administration: Oral Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance.Plasma protein binding was 1% in rat and human plasma.
保存条件：-20℃

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