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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]}
批次查询： 批次纯度:

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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 2HCl ✔ 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 ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
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

    rat H3 receptor, Ki:1.44 μM

    human H3 receptor, Ki:1.2 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 288.38
SMILES Code O=C(N)C1=CC=C(OCCCN2CC3C(CCC3)C2)C=C1
MDL No. MFCD31560487
别名
运输蓝冰
InChI Key MRNMYWNBLVJWKG-UHFFFAOYSA-N
Pubchem ID 11380684
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

Tags: S 38093 | 862896-30-8 | S38093 | S-38093 | H3 Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | S 38093 纯度/质量文件 | S 38093 亚型比较 | S 38093 生物活性 | S 38093 参考文献 | S 38093 实验方案 | S 38093 技术信息

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