Powder: -20°C for 3 years | In solvent: -80°C for 1 year
S 38093 是一种可透过大脑的,可口服的组胺 H3 受体拮抗剂,对大小鼠和人的 H3 受体具有不同的亲和力,Ki 值分别为 8.8、1.44 和 1.2 µM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 398 | 现货 | ||
2 mg | ¥ 543 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 957 | 现货 | ||
25 mg | ¥ 1,820 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,770 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 758 | 现货 |
产品描述 | S 38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8/1.44/1.2 μM, for rat/mouse/human). |
靶点活性 | H3 receptor (mouse):1.44 μM(Ki), H3 receptor (rat):8.8 μM(Ki), H3 receptor (human):1.2 μM(Ki) |
体外活性 | In cellular models, S 38093 can antagonize mice H3 receptors (KB: 0.65 μM) and suppress cAMP decrease induced by an H3 agonist (KB: 0.11 μM). In cells expressing a high H3 density, S 38093 is a moderate inverse agonist at the rat and human H3 receptors (EC50: 9/1.7 μM, respectively)[2]. |
体内活性 | In young adult mice, S 38093 (0.3/3?mg/kg/day, p.o., 28 days) markedly increases proliferation of progenitors in the DG of the hippocampus. S 38093 (0.3?mg/kg/day) markedly increases the number of DCX+?cells with tertiary dendrites. S 38093 (0.3/1/3?mg/kg) markedly increases cell survival, proliferation, and maturation in the DG of the hippocampus in aged mice relative to the vehicle. S 38093 (3?mg/kg/day, p.o., 28 days) increases cell proliferation and has a strong effect on cell survival, also increases the dendritic intersections in both genotypes, with a significant effect from 50 to 80 in APPSWETG?mice only. In aged mice, chronic administration of S 38093 (1/3?mg/kg/day, p.o., 28 days) reverses this age-dependent decrease in BDNF-IX/IV/I transcripts. In addition, S 38093 at three tested doses (0.3/1/3?mg/kg/day) increases VEGF transcripts compared to the vehicle-aged group[1]. |
动物实验 | S 38093 is formulated in purified water.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. 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 0.75?mA 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 olf |
别名 | S38093, S-38093 |
分子量 | 288.38 |
分子式 | C17H24N2O2 |
CAS No. | 862896-30-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (190.72 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.4676 mL | 17.3382 mL | 34.6765 mL | 86.6912 mL |
5 mM | 0.6935 mL | 3.4676 mL | 6.9353 mL | 17.3382 mL | |
10 mM | 0.3468 mL | 1.7338 mL | 3.4676 mL | 8.6691 mL | |
20 mM | 0.1734 mL | 0.8669 mL | 1.7338 mL | 4.3346 mL | |
50 mM | 0.0694 mL | 0.3468 mL | 0.6935 mL | 1.7338 mL | |
100 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8669 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
S 38093 862896-30-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor inhibit S38093 S-38093 Inhibitor inhibitor