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S 38093

S 38093

产品编号 T4099   CAS 862896-30-8
别名: S38093, S-38093

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。

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S 38093 Chemical Structure
S 38093, CAS 862896-30-8
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
其他形式的 S 38093:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: S 38093 (T4099)
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (190.72 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Guilloux JP, et al. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. 2. Sors A, et al. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23
Cinnarizine N-Acetylhistamine acetate DREADD agonist 21 H4R antagonist 1 Ziprasidone PF-03654746 Tosylate Asenapine ST-1006

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗癌临床化合物库 神经退行性疾病化合物库 GPCR靶点分子库 抗癌药物库 抑制剂库 膜蛋白靶向化合物库 NO PAINS 化合物库 已知活性化合物库 血脑屏障通透化合物库

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Keywords

S 38093 862896-30-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor inhibit S38093 S-38093 Inhibitor inhibitor

 

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