| 中文名称: | GSK1059865 | ||||
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| 英文名称: | GSK1059865 | ||||
| 别名: | [(2S,5S)-2-[[(5-Bromopyridin-2-yl)amino]methyl]-5-methylpiperidin-1-yl]-(3-fluoro-2-methoxyphenyl)methanone | ||||
| CAS No: | 1191044-58-2 | 分子式: | C20H23BrFN3O2 | 分子量: | 436.32 |
| CAS No: | 1191044-58-2 | ||||
| 分子式: | C20H23BrFN3O2 | ||||
| 分子量: | 436.32 | ||||
基本信息
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产品编号： |
G10768 |
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产品名称： |
GSK1059865 |
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CAS: |
1191044-58-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
436.32 |
-20℃ |
1个月 |
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化学名： |
[(2S,5S)-2-[[(5-Bromopyridin-2-yl)amino]methyl]-5-methylpiperidin-1-yl]-(3-fluoro-2-methoxyphenyl)methanone |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.2919mL |
11.4595mL |
22.9190mL |
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5mM |
0.4584mL |
2.2919mL |
4.5838mL |
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10mM |
0.2292mL |
1.1459mL |
2.2919mL |
生物活性
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产品描述 |
一种有效地食欲素1受体 (orexin 1 receptor) 拮抗剂。 |
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靶点 |
Orexin 1 receptor |
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体内研究 |
Treatment with GSK1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice.In contrast GSK1059865 decreases drinking in air-exposed mice only at the highest dose used.There is no effect of GSK1059865 on sucrose intake.GSK1059865 (0.3nM 10nM) produces non-surmountable antagonism with a dosedependent rightward shift of the OXA EC50 and a concomitant decrease of the agonist maximal response.The calculated pKB value is 8.77±0.12 for GSK1059865.GSK1059865 (0.1-3.3μM) produces a classical surmountable profile with parallel rightward shift of the OXA EC50 without depression of the agonist maximal response.Intraperitoneal administration of GSK1059865 produces a region-dependent inhibition of yohimbine-induced relative cerebral blood volume response.The administration of GSK1059865 per se produces a weak relative cerebral blood volume increase in several brain regions.GSK1059865-pretreated animals exhibit slightly higher baseline mean arterial blood pressure values than controls. |
推荐实验方法(仅供参考)
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动物实验: |
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Rats:GSK1059865 is dissolved in 0.5% HPMC (w/v) in distilled water and administered by gavage at doses of 10 and 30mg/kg to rats.Drug or vehicle is administered 1h before access to highly palatable food. Mice:During baseline and the first 5 test cycles following chronic intermittent ethanol (or air) exposure,mice receive vehicle (saline) injections (i.p.;0.01ml/g body weight) 30 minutes before drinking ethanol.On test cycles 6 and 7 mice receive vehicle or GSK1059865 (10,25,50mg/kg) before given access to ethanol 15% v/v (Test 6) or sucrose 5% w/v (Test 7) versus water.GSK1059865 is dissolved in saline and TWEEN 80 (0.5 % v/v) as vehicle. |
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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 )
