中文名稱:化合物 PF8380 | 英文名稱:PF-8380 |
CAS:1144035-53-9 | 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: 99.45% | 產(chǎn)品類別: 抑制劑 |
貨號: T3631 |
名稱 | PF-8380 |
描述 | PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysophosphatidic acid (LPA) levels in vivo/vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at the site of inflammation. |
細胞實驗 | GL261 or U87-MG cells are plated in triplicate onto 6 cm plates and allowed to grow to 70% confluence. The semi-confluent cell layer is scratched with a sterile 200 μL pipette tip to create a scratch devoid of cells and plates are washed once with PBS to remove non-adherent cells and debris. For radiosensitization drug studies, cells are treated with 1 μM PF-8380 or DMSO for 45 min prior to irradiation with 4 Gy, and then incubated at 37°C in 5% CO2. Control plates are monitored for cell migration (20–24 h). Cells are fixed with 70% ethanol and stained with 1% methylene blue. To quantify migration, cells in three randomly selected high power fields (HPFs) in the scratched area are counted and normalized for surrounding cell density.(Only for Reference) |
激酶實驗 | FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1]. |
體外活性 | 在放射輻射前,PF-8380預處理可抑制輻射誘導的腫瘤血管內(nèi)皮細胞血管生成、并延遲神體內(nèi)經(jīng)膠質(zhì)瘤腫瘤生長與發(fā)展[2]. 在大鼠氣囊炎模型中,PF8380(30 mg/kg,p.o.)可減少炎性痛覺過敏,3 h內(nèi)可使血漿和炎癥組織的LPA水平降低超過95%. |
體內(nèi)活性 | PF-8380與FS-3D底物抑制大鼠自毒素(IC50:1.16 nM)。在人體全血中,PF-8380處理2 h可抑制自毒素(IC50:101 nM)[1]。PF-8380可抑制GBM細胞的自毒素,隨后使其入侵及遷移減少、并使輻射敏化增強。 |
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 : <1 mg/mL (insoluble or slightly soluble) |
關鍵字 | inhibit | Phosphodiesterase (PDE) | PF 8380 | PF8380 | PF-8380 | Inhibitor |
相關產(chǎn)品 | Icariin | Vardenafil hydrochloride | Apremilast | Indomethacin | Roflumilast | Theophylline | Acefylline | Theobromine | Theophylline monohydrate | Isoprenaline hydrochloride | Diphylline | Doxofylline |
相關庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 活性脂質(zhì)化合物庫 | 抗阿爾茨海默癥化合物庫 | 抗心血管疾病化合物庫 | 抗COVID-19化合物庫 | NO PAINS 化合物庫 | 神經(jīng)退行性疾病化合物庫 | 抗代謝疾病化合物庫 |
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 |
產(chǎn)品名稱 | 價格 | 公司名稱 | 報價日期 | |
---|---|---|---|---|
詢價 |
VIP1年
|
上海逐耀醫(yī)藥科技有限公司
|
2024-11-07 | |
¥5651.90 |
VIP13年
|
上海阿拉丁生化科技股份有限公司
|
2024-10-31 | |
詢價 |
VIP4年
|
河源廣譜生物技術有限公司
|
2024-10-31 | |
詢價 |
VIP9年
|
上海芮暉化工科技有限公司
|
2024-09-04 | |
¥2906.71 |
VIP10年
|
西格瑪奧德里奇(上海)貿(mào)易有限公司
|
2023-10-27 |