货号: | T4099 |
供应商: | TargetMol中国 |
数量: | 大量 |
英文名: | S-38093 |
保质期: | 干粉三年 |
保存条件: | -20°C |
规格: | 1mg/2mg/5mg/10mg/20mg/50mg/100mg/200mg/10mM * 1mL (in DMSO) |
美国进口,中国现货
溶解度Solubility:15mg/mL in DMSO
Pathways:GPCR/G Protein; Immunology/Inflammation; Neuroscience
Target:Histamine Receptor antagonist
Receptor:Human H3 receptor; Mouse H3 receptor; Rat H3 receptor
Bioactivity:S38093 is a brain-penetrant antagonist of H3 receptor, with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
体外实验:In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65 µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11 µM). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7 µM, respectively)[2].
体内实验:S 38093 (0.3 and 3 mg/kg/d p.o., 28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice. S 38093 (0.3 mg/kg/d) treatment significantly increases the number of DCX+ cells with tertiary dendrites. S 38093 (0.3, 1 and/or 3 mg/kg) significantly increases cell proliferation, survival, and maturation in the DG of hippocampus in aged mice relative to vehicle. S 38093 (3 mg/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 3 mg/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 3 mg/kg/d) increases VEGF transcripts compared to vehicle-aged group[1]. In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3 mg/kg p.o. and antagonized R-α-Methylhistamine-induced dipsogenia from 10 mg/kg i.p[2].
更多产品信息,请点击:http://www.tsbiochem.com/productview/s-38093.html
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