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 |
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 | 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 |
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,相比于對照組。S 38093(3 mg/kg/天,口服,28天)提高了細(xì)胞增殖,并對細(xì)胞存活產(chǎn)生強(qiáng)烈影響,也增加了兩種基因型的樹突交叉點(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,與老齡對照組相比,S 38093在三個(gè)測試劑量(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 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | GPCR靶點(diǎn)分子庫 | 膜蛋白靶向化合物庫 | 神經(jīng)退行性疾病化合物庫 | 藥物功能重定位化合物庫 | 疼痛相關(guān)化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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