中文名称: | Lesogaberan | ||||
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英文名称: | Lesogaberan | ||||
别名: | Lesogaberan AZD-3355 | ||||
CAS No: | 344413-67-8 | 分子式: | C3H9FNO2P | 分子量: | 141.08 |
CAS No: | 344413-67-8 | ||||
分子式: | C3H9FNO2P | ||||
分子量: | 141.08 |
基本信息
产品编号: |
L10500 |
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产品名称: |
Lesogaberan |
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CAS: |
344413-67-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
二年 |
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分子量: |
141.08 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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 |
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靶点 |
Ki:5.1±1.2nM (rat GABAB),1.4±0.3μM (rat GABAA) EC50:8.6±0.77nM (human GABAB receptor) |
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体外研究 |
Lesogaberan (3-30nM) enhances human islet cell proliferation in vitro. Cell Proliferation Assay |
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Cell Line: |
Human islet cells |
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Concentration: |
3,10,and 30nM |
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Incubation Time: |
4 days |
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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. |
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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. |
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Animal Model: |
Diabetic NOD/scid mice were implanted with human islets |
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Dosage: |
0.08mg/mL |
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Administration: |
Oral feeding;48 hours |
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Result: |
Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+β-cells in human islet grafts. |
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Animal Model: |
Female Sprague Dawley rats |
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Dosage: |
7μmol/kg (Pharmacokinetic Analysis) |
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Administration: |
Oral |
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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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )