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S 38093 {[allProObj[0].p_purity_real_show]}

货号:A642303

S 38093是一种可穿透大脑的H3受体拮抗剂/反向激动剂。它对大鼠、小鼠和人源H3受体具有不同的亲和力,Ki值分别为8.8、1.44和1.2 µM。此化合物对其他组胺能受体没有亲和力。

S 38093 化学结构 CAS号:862896-30-8
S 38093 化学结构
CAS号:862896-30-8
S 38093 3D分子结构
CAS号:862896-30-8
S 38093 化学结构 CAS号:862896-30-8
S 38093 3D分子结构 CAS号:862896-30-8
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S 38093 纯度/质量文件 产品仅供科研

货号:A642303 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 99%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

S 38093 生物活性

靶点
  • H3 receptor

    human H3 receptor, Ki:1.2 μM

    rat H3 receptor, Ki:1.44 μM

描述 S 38093 is a novel Histamine H3 receptor inverse agonist with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively[1]. S 38093 (0.3, 1 and/or 3 mg/kg) significantly increased cell proliferation, survival, and maturation in the dentate gyrus of hippocampus in aged mice relative to vehicle, and high doses of S 38093 also increased the maturation of newborn neurons. Chronic administration of S 38093 (3 mg/kg/d p.o., 28 days) administration also increased the dendritic intersections in Alzheimer’s disease transgenic mice: APPSWEWT and APPSWETg[2]. Donepezil and S 38093 (at 0.1, 0.3, and 1.0 mg/kg) induced a dose-dependent synergistic memory-enhancing effect in middle-aged mice, which is mediated by its action on the septo-hippocampal circuitry, since it canceled out the reduction of CREB phosphorylation (pCREB) observed in these brain areas in vehicle-treated middle-aged animals[3].

S 38093 参考文献

[1]Sors A, Panayi F, Bert L, et al. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017;803:11‐23.

[2]Guilloux JP, Samuels BA, Mendez-David I, et al. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017;7:42946.

[3]Sors A, Krazem A, Kehr J, et al. The Synergistic Enhancing-Memory Effect of Donepezil and S 38093 (a Histamine H3 Antagonist) Is Mediated by Increased Neural Activity in the Septo-hippocampal Circuitry in Middle-Aged Mice. Front Pharmacol. 2016;7:492.

S 38093 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.47mL

0.69mL

0.35mL

17.34mL

3.47mL

1.73mL

34.68mL

6.94mL

3.47mL

S 38093 技术信息

CAS号862896-30-8
分子式C17H24N2O2
分子量 288.385
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 2 mg/mL(6.94 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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