化合物 S38093|T4099|TargetMol

價(jià)格	￥398	￥543	￥747
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 S38093	英文名稱:S 38093
CAS:862896-30-8	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.98%	產(chǎn)品類別: 抑制劑
貨號(hào): T4099

Product Introduction

Bioactivity

名稱	S 38093
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).
動(dòng)物實(shí)驗(yàn)	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
體外活性	在細(xì)胞模型中，S 38093能夠拮抗小鼠H3受體(KB: 0.65 μM)，并且能夠抑制由H3激動(dòng)劑引起的cAMP降低(KB: 0.11 μM)。在表達(dá)高密度H3受體的細(xì)胞中，S 38093對(duì)大鼠和人類H3受體表現(xiàn)為中等強(qiáng)度的反向激動(dòng)作用（EC50: 分別為9/1.7 μM）[2]。
體內(nèi)活性	在年輕成年小鼠中，S 38093（0.3/3 mg/kg/天，口服，28天）顯著增加了海馬齒狀回（DG）內(nèi)前體細(xì)胞的增殖。S 38093（0.3 mg/kg/天）顯著增加具有第三級(jí)樹(shù)突的DCX+細(xì)胞數(shù)量。S 38093（0.3/1/3 mg/kg）顯著提高老年小鼠海馬DG中細(xì)胞的存活、增殖和成熟，相比于對(duì)照組。S 38093（3 mg/kg/天，口服，28天）提高了細(xì)胞增殖，并對(duì)細(xì)胞存活產(chǎn)生強(qiáng)烈影響，也增加了兩種基因型的樹(shù)突交叉點(diǎn)，僅在APPSWETG小鼠中從50至80有顯著效果。在老年小鼠中，S 38093的長(zhǎng)期給藥（1/3 mg/kg/天，口服，28天）逆轉(zhuǎn)了這種與年齡相關(guān)的BDNF-IX/IV/I轉(zhuǎn)錄本的減少。此外，與老齡對(duì)照組相比，S 38093在三個(gè)測(cè)試劑量（0.3/1/3 mg/kg/天）均增加了VEGF轉(zhuǎn)錄本[1]。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (190.72 mM)
關(guān)鍵字	inhibit \| S 38093 \| Histamine Receptor \| Inhibitor
相關(guān)產(chǎn)品	Famotidine \| Meclizine dihydrochloride \| Nizatidine \| Lidocaine \| Sodium butanoate \| Alginic acid \| Mirtazapine \| Amitriptyline hydrochloride \| Trazodone hydrochloride \| Mianserin hydrochloride \| Doxepin hydrochloride \| Chlorphenesin
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| GPCR靶點(diǎn)分子庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 神經(jīng)退行性疾病化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： S-38093|||S38093|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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公司成立：12年
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