| 中文名称: | AR-M 1000390 hydrochloride | ||||
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| 英文名称: | AR-M 1000390 hydrochloride | ||||
| 别名: | N,N-二乙基-4-(苯基-4-哌啶基甲基)苯甲酰胺盐酸盐 N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride | ||||
| CAS No: | 209808-47-9 | 分子式: | C23H29ClN2O | 分子量: | 384.94 |
| CAS No: | 209808-47-9 | ||||
| 分子式: | C23H29ClN2O | ||||
| 分子量: | 384.94 | ||||
基本信息
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产品编号： |
A12778 |
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产品名称： |
AR-M 1000390 hydrochloride |
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CAS: |
209808-47-9 |
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： |
384.94 |
-20℃ |
1个月 |
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化学名： |
N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride |
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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 |
2.5978mL |
12.9890mL |
25.9781mL |
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5mM |
0.5196mL |
2.5978mL |
5.1956mL |
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10mM |
0.2598mL |
1.2989mL |
2.5978mL |
生物活性
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产品描述 |
一种有效的选择性δ阿片受体激动剂，EC50为7.2±0.9nM。 |
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靶点 |
EC50:7.2±0.9nM (δ opioid receptor) |
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体外研究 |
AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC50) of 0.87±0.23nM for the δopioid receptor and extremely high selectivity over the µ receptor (IC50=3800±172nM) and the κ receptor (IC50=7470±606nM).RINm5F cells are treated with AR-M 1000390 (AR-M100390) and Cyclizine for 16-24h before measurement of intracellular and secreted insulin levels.AR-M 1000390 mediates a dose-dependent decrease in insulin content with a maximal inhibition of ~90% at the highest concentration tested (10μM). |
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体内研究 |
Rats are treated with 5,100,and 600μmol/kg of AR-M 1000390 (AR-M100390) for 3 and/or 7 days;another group of rats treated with 600μmol/kg of compound are allowed to recover for 14 days.AR-M 1000390 (600μmol/kg) causes vacuolation in the β-cell of the rat pancreas that is associated with depletion of insulin and hyperglycemia after 7 days of dosing.Treatment of rats with 600μmol/kg of AR-M 1000390 results in vacuolation of the β-cell of the rat pancreas that is similar to that reported for cyclizine and cyproheptadine. |
推荐实验方法(仅供参考)
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细胞实验: |
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RINm5F cells are seeded in 24-well plates and treated with vehicle (DMSO),10μM AR-M 1000390 (AR-M100390),and 10μM Cyclizine in serum-free medium;cells are rinsed with phosphate-buffered saline and stored at -80℃ until analysis. RNA is isolated with the RNeasy purification system with DNAse treatment. |
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动物实验: |
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Rats Han Wistar rats (six per treatment group) are treated with vehicle (saline) or 5,100,and 600μmol/kg/day of AR-M 1000390 (AR-M100390) for 7 days.A separate group of rats are treated with 600μmol/kg/day for 7 days followed by a 14-day recovery period.Another group is treated with 600μmol/kg/day for 3 days.Blood sampling for glucose,lipids,and insulin measurements are taken on days 2,4,8,and 22.Blood sampling for AR-M 1000390 concentration measurements are collected on days 4 and 8.The animals are euthanized with CO2 on days 4,8,and 22 and the pancreas isolated and processed for histopathology,insulin immunohistochemistry,and insulin mRNA analyses. |
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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 )
