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Lesogaberan hydrochloride

    
10mM in DMSO

源叶(MedMol)
V58293 一键复制产品信息
2925644-17-1
C3H10ClFNO2P
177.54
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V58293-1ml
10mM in DMSO

¥3350.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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
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参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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