價格 | ¥262 | ¥430 | ¥795 |
包裝 | 5mg | 10mg | 25mg |
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 JZL184 | 英文名稱:JZL 184 |
CAS:1101854-58-3 | 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: 97.89% | 產(chǎn)品類別: 抑制劑 |
貨號: T6554 |
名稱 | JZL 184 |
描述 | JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively. |
細(xì)胞實(shí)驗(yàn) | 1 × 105 cells are split into four-well chamber slides and incubated with culture medium containing BrdU for 4 h. BrdU staining is performed following the manufacturer's instructions.(Only for Reference) |
激酶實(shí)驗(yàn) | activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s |
體外活性 | JZL184是研究內(nèi)源性2-AG信號效應(yīng)的有用工具。JZL184展現(xiàn)出對MAGL的時間依賴性抑制作用,并在體外對MAGL比FAAH具有超過300倍的選擇性。JZL184不與CB1或CB2受體相互作用,也不抑制2-AG生物合成酶二?;视椭?α和二?;视椭?β,或花生四烯酸動員酶胞漿磷脂酸A2群IVA。[1] |
體內(nèi)活性 | JZL184在小鼠大腦中迅速且持續(xù)地阻斷了2-AG水解酶活性,導(dǎo)致內(nèi)源性2-AG水平升高8倍,并至少維持8小時。接受JZL184處理的小鼠表現(xiàn)出一系列CB1依賴的行為效應(yīng),包括鎮(zhèn)痛、運(yùn)動減少和低體溫,這表明2-AG介導(dǎo)的內(nèi)源性大麻素信號在整個哺乳動物神經(jīng)系統(tǒng)中具有廣泛作用。[1] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 93 mg/mL (178.7 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | MAGL | neurons | inhibit | 2-Arachidonoylglycerol | JZL-184 | Inhibitor | hydrolysis | Monoacylglycerol lipase | analgesia | JZL 184 | antinociceptive |
相關(guān)產(chǎn)品 | euphol | Endothelial lipase inhibitor-1 | XEN445 | Atglistatin | JNJ-42226314 | KML29 | WWL70 | Lalistat 2 | ABX-1431 | JJKK 048 | NG-497 | Beta-Sitosterol |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 代謝化合物庫 | 活性脂質(zhì)化合物庫 | 高選擇性抑制劑庫 | NO PAINS 化合物庫 | 抗肥胖化合物庫 | 抗代謝疾病化合物庫 | 共價抑制劑庫 |
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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