S 38093

製品コードS8598 バッチS859801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H24N2O2
分子量 288.38 CAS No. 862896-30-8
Solubility (25°C)* 体外 DMSO 57 mg/mL (197.65 mM)
Ethanol 57 mg/mL (197.65 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 S 38093は、ラット、マウス、ヒトのH3受容体に対して中程度の親和性を持つヒスタミンH3アンタゴニスト/インバースアゴニストであり（Ki = それぞれ8.8、1.44、1.2 μM）、他のヒスタミン作動性受容体には親和性がありません。
in vitro In cellular models, this compound was 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). Among the four histaminergic receptor subtypes, it is selective for the H3 receptor, its binding affinity for H1, H2 and H4 receptors being negligible.
in vivo S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturation and survival) in 3-month-old and in aged 16-month-old mice. In aged animals, this compound induced a reversal of age-dependent effects on hippocampal brain-derived neurotrophic factor (BDNF) BDNF-IX, BDNF-IV and BDNF-I transcripts and increased vascular endothelial growth factor (VEGF) expression. The effects of chronic administration of this compound were assessed on a neurogenesis-dependent “context discrimination (CS) test” in aged mice. While ageing altered mouse CS, chronic treatment with this chemical significantly improved CS. Chronic treatment with this compound increases adult hippocampal neurogenesis and may provide an innovative strategy to improve age-associated cognitive deficits. This compound is found to be active at a mean pharmacological dose of 0.3–1 mg/kg p.o./i.p. in animal behavioral tests of working memory (Morris water maze in rats; spontaneous alternation and concurrent serial alternation tests in mice; delayed matching to sample in aged monkeys) and episodic-like memory (social and object recognition tests in rats; contextual discrimination task in mice). It also improves attention, executive functioning, and cognitive flexibility in MPTP-treated monkeys. Moreover, in line with its H3 antagonist/inverse agonist properties, this chemical dose-dependently increases extracellular histamine levels in the prefrontal cortex and facilitates cholinergic transmission in the prefrontal cortex and hippocampus of rats after both acute and chronic administrations. This compound was rapidly absorbed in mouse and rat (Tmax= 0.25-0.5h), slowly in monkey (2h), with a bioavailability ranging from 20 to 60% and t1/2 ranging from 1.5h to 7.4h. The compound was widely distributed with a moderate volume of distribution and low protein binding. The brain distribution of this chemical was rapid and high.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK-293 cells
濃度 0.01-100 μM
反応時間 1 h
実験の流れ

The cells (2 x 106 per ml) were harvested and suspended in Hank's balanced salt solutions/HEPES (pH7.4) buffer containing 1 mM isobutyl-methylxanthine and 1mg/ml of BSA. The fluor 647-anti cAMP antibody solution (1 μl) was added to the cell suspension (100 μl) and 6 μl aliquots of this mix were dispensed in white 384-well microtiter plates. The cells were then incubated with 6 μl aliquots of S 38093 and/or the reference compounds (specific H3 agonist Imetit or antagonist Thioperamide) at increasing concentrations (0.01-100 μM), in the presence of forskolin (FSK, 0.5 μM final concentration) in order to preactivate adenylate cyclase. After a 1 h incubation at room temperature in the dark, the lysis buffer (0.35% Triton X-100, 10mM CaCl2, 50mM HEPES) containing LANCE EU-W8044 labeled streptavidin and biotinyled cAMP was added to the cells. After a 20 h incubation at + 4°C in the dark, plates were read on an microplate reader.
動物実験 動物モデル C57Bl/6JRj male mice
投薬量 0.3, 1 and 3 mg/kg/day
投与方法 p.o

参考

  • https://pubmed.ncbi.nlm.nih.gov/28336400/
  • https://pubmed.ncbi.nlm.nih.gov/28218311/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。