中文名稱:塞來昔布 | 英文名稱:Celecoxib |
CAS:169590-42-5 | 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: T0466 |
名稱 | Celecoxib |
描述 | Celecoxib (SC 58635) is a non-steroidal anti-inflammatory agent, a COX-2 inhibitor (IC50=40 nM), with selectivity. Celecoxib has anti-inflammatory and analgesic activity and can be used for the treatment of osteoarthritis, rheumatoid arthritis, and acute pain. |
細胞實驗 | The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.(Only for Reference) |
激酶實驗 | COX enzyme assay in vitro: Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation. |
體外活性 | 方法:鼻咽癌 (NPC) 細胞系 HNE1 和 CNE1-LMP1 用 Celecoxib (5-75 μM) 處理 48 h,使用 MTT assay 檢測細胞活力。 結(jié)果:Celecoxib 的抑制作用以劑量依賴的方式發(fā)生。Celecoxib 在 HNE1 和 CNE1-LMP1 中的平均 IC50 值分別為 32.86±1.13 μmol/L 和 61.31±4.30 μmol/L。[1] 方法:人正常肝細胞 L02 用 PA (200 μM) 和 Celecoxib (5-40 μM) 處理 24 h,使用 Western Blot 檢測靶點蛋白表達水平。 結(jié)果:PA 誘導 COX-2 上調(diào),LC3 II/I 和 p62 的蛋白質(zhì)表達增加。PA和 Celecoxib 聯(lián)用,COX-2 和 p62 的蛋白水平顯著降低,LC3 II/I 增加。[2] |
體內(nèi)活性 | 方法:為測試是否能降低放射性肺炎的死亡率,將 Celecoxib (25 ?mg/kg in 0.5% methyl cellulose and 0.025% Tween 20 in sterile water) 灌胃給藥給局部胸部照射 (LTI) 的 C3Hf/KamLaw 小鼠。從 LTI 當天或 40 或 80 天后開始給藥,每天兩次,持續(xù)四十天。 結(jié)果:Celecoxib 相對于 LTI 的時間決定了療效。只有當 Celecoxib 在 LTI 后 80 天開始使用時,死亡時間才能顯著縮短,這與肺炎的表達時間相對應(yīng)。對于這些小鼠,死亡率的降低被量化為治療組與未治療組的死亡率的風險比為 0.36。[3] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.1 mg/mL (18.62 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : 31 mg/mL (81.3 mM) 2% DMSO+40% PEG300+5% Tween 80+53% H2O : 3 mg/mL (7.87 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 60 mg/mL (157.33 mM) |
關(guān)鍵字 | inhibit | Inhibitor | COX | Celecoxib | Cyclooxygenase | SC-58635 | SC58635 |
相關(guān)產(chǎn)品 | Revaprazan hydrochloride | Ibuprofen | Paradol | Glafenine | trans-Cinnamaldehyde | Acetaminophen | Diclofenac Potassium | Indomethacin sodium hydrate | Salicylamide | Salicylic acid | Bismuth Subsalicylate | Diclofenac sodium |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | EMA 上市藥物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 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 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務(wù) |
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