| 中文名称: | S 38093 | ||||
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| 英文名称: | S 38093 | ||||
| 别名: | 4-(3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide | ||||
| CAS No: | 862896-30-8 | 分子式: | C17H24N2O2 | 分子量: | 288.391 |
| CAS No: | 862896-30-8 | ||||
| 分子式: | C17H24N2O2 | ||||
| 分子量: | 288.391 | ||||
基本信息
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产品编号： |
S10050 |
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产品名称： |
S 38093 |
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CAS: |
1222097-72-4 |
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： |
288.39 |
-20℃ |
1个月 |
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化学名： |
4-(3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide |
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Solubility (25°C)： |
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体外:
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DMSO |
57mg/mL (197.65mM) |
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Ethanol |
57mg/mL (197.65mM) |
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Water |
Insoluble |
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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 |
3.4676mL |
17.3382mL |
34.6765mL |
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5mM |
0.6935mL |
3.4676mL |
6.9353mL |
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10mM |
0.3468mL |
1.7338mL |
3.4676mL |
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50mM |
0.0694mL |
0.3468mL |
0.6935mL |
生物活性
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产品描述 |
一种组胺H3受体的反向激动剂。 |
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靶点 |
Ki:8.8µM (Rat H3 receptor),1.44µM (Mouse H3 receptor),1.2µM (Human H3 receptor) |
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体外研究 |
In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11µM).In cells expressing a high H3 density,S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7µM,respectively). |
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体内研究 |
S 38093 (0.3 and 3mg/kg/d p.o.,28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice.S 38093 (0.3mg/kg/d) treatment significantly increases the number of DCX+cells with tertiary dendrites. S 38093 (0.3,1 and/or 3mg/kg) significantly increases cell proliferation,survival,and maturation in the DG of hippocampus in aged mice relative to vehicle.S 38093 (3mg/kg/d p.o.,28 days) increases cell proliferation and has a strong effect on cell survival,also increases the dendritic intersections in both genotypes (one-way ANOVA with repeated measure,p < 0.01), with a significant effect from 50 to 80 in APPSWETG mice only. In aged mice,chronic administration of S 38093 (1 and/or 3mg/kg/day p.o.,28 days) reverses this age-dependent decrease in BDNF-IX,BDNF-IV and BDNF-I transcripts.In addition,S 38093 at three tested doses (0.3,1 and 3mg/kg/d) increases VEGF transcripts compared to vehicle-aged group.In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3mg/kg p.o.and antagonized R-αMethylhistamine-induced dipsogenia from 10mg/kg i.p. |
推荐实验方法(仅供参考)
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细胞实验: |
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细胞系 |
HEK-293 cells |
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浓度 |
0.01-100μM |
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处理时间 |
1h |
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方法 |
收集细胞，并以2x106/ml的密度悬浮于含1mM isobutyl-methylxanthine和1mg/ml BSA的Hank's balanced salt solutions/HEPES (pH7.4) buffer中。向其中加入1μL fluor 647-anti cAMP antibody solution，混合好后，将溶液分装于384孔板（6μL每份）。加入S38093和/或其他化合物（0.01-100μM），加入终浓度为0.5μM FSK以预激活腺甘酸环化酶。在黑暗条件下常温孵育1小时，加入含LANCE EU-W8044 labeled streptavidin和biotinyled cAMP的lysis buffer，黑暗、4℃下孵育20小时。酶标仪检测。 |
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动物实验: |
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The context discrimination task consists of an 8-day contextual fear discrimination paradigm in which the mice have to learn to distinguish between a fearful shock context and a similar non-shock context.On day 1 the mice are only exposed to the training shock context,and on days 2-8 the mice are exposed to the shock and then non-shock context in that order each day.The mice are run through the context discrimination task starting at 10 am and ending at 2 pm and are then gavaged with vehicle or S 38093 at 4 pm each day.The drug and vehicle are always administered after behavioral testing to avoid possible acute effects of the drug on behavior.Learning is measured by the percent time the mice spent freezing and testing is terminated when percent freezing is consistently significantly different between the two contexts.The mice are tested after 29 days of drug treatment. Conditioning is conducted on one side of a Med-Associates shuttle box (ENV-010MC;20.3 cm×15.9 cm×21.3 cm high) with a clear plexiglass wall,3 aluminum walls and a stainless steel grid as a floor.Mouse behavior is recorded by digital video cameras mounted above the conditioning chamber.Freezeframe and Freezeview softwar are used for recording and analyzing freezing behavior,respectively. In training context A,mice are allowed to habituate in new cages outside the room and are then brought into the room in the new cages.The house fan and house light are turned on,the stainless steel grid is exposed,the plexiglass wall is up and a mild anise scent is used as an olfactory cue.The door to the sound dampening enclosure is shut for the duration of the trial.180 s after the mice are placed in the training context,they are delivered a single footshock of 0.75mA lasting 2 s.15 s after the end of the footshock,the mice are placed back into their home cages.Non-alcoholic antiseptic wipes are used to clean the grids and catch trays in between trials.An hour later the mice are brought into the room in paper buckets and put into similar context B.The house fan and house light are turned off,the door of the enclosure is left ajar,plastic placemat sheets are put into the shuttle box to make a high-walled circular enclosure,the plexiglass wall is left down and a mild lemon scent is used as the olfactory cue.The stainless steel grid,a salient feature of both contexts,remained exposed. The mice stayed in the chambers for 180s without receiving a footshock and are placed back into their home cages.70% ethanol is used to clean the grids and catch trays between trials.The discrimination ratio allowed for evaluation of discrimination between the two contexts and is computed as follows:A = freezing in context A,B= freezing in context B,and the discrimination ratio = A/(A+B).Larger values indicate better discrimination. |
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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 )
