布洛芬 T1394

Product Introduction
Bioactivity


英文名: Ibuprofen

描述: Ibuprofen (Advil) 是一种丙酸衍生物和非甾体抗炎药 (NSAID)，具有抗炎、镇痛和解热作用。它是COX-1和COX-2的抑制剂，IC50值分别为 13 和 370 μM，导致前列腺素和血栓素前体的形成减少。

细胞实验: Each cell line is incubated with Ibuprofen of various concentrations for 48 hours. Cell survival is estimated by the MTT assay, and cell death is determined by Hoechst staining used to distinguish between intact cell nuclei and fragmented nuclei undergoing cell death. Cells are lysed and analyzed by western blotting for detection of the p75NTR protein.(Only for Reference)

激酶实验: Radiochemical enzyme assays for COX-1 and COX-2: 10 μL of purified COX-1 (0.7-0.8 μg) or COX-2 (3.0 units, 0.3μg) is activated with 50 μL of cofactor solution [l-epinephrine (1.3 mg/mL), reduced glutathione (0.3 mg/mL), and hematin (1.3 mg/mL) in oxygen-free Tris-HCl buffer (pH 8.0)]. The enzyme solution (60 μL) is added to Ibuprofen solutions or DMSO (20 μL) after [14C]arachidonic acid is added in 0.2 mL eight-strip test tubes and preincubated 10 minutes on ice. Samples are incubated for 15 minutes at 37 °C, after which the reaction is terminated by addition of 10 μL of 2 M HCl and 5 μL of carrier solution (PGE2 and PGF2α, 0.2 μg/mL of each in EtOH). The unmetabolized arachidonic acid is separated from the prostaglandin products by column chromatography and eluted with n-hexane-dioxane-glacial acetic acid (70:30:1). The prostaglandin products are then eluted with EtOAc-MeOH (85:15), and the samples are counted in a Packard scintillation spectrometer. IC50 values are obtained by linear regression analysis.

体外活性: 在HRHF方式诱导的成年雌性Sprague-Dawley大鼠模型中,Ibuprofen通过阻断血清C1和2C以及胶原降解与合成,治疗关节炎症和早期关节软骨退变.

体内活性: 在细胞中,Ibuprofen能够抑制环氧合酶COX-1和COX-2,及花生四烯酸转换为前列腺素H2 (PGH2)。在前列腺肿瘤细胞,Ibuprofen能够抑制NF-κB和IKKα的激活。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (266.63 mM)
Ethanol : 39 mg/mL (189.1 mM)


关键字: AGS | gastric cancer | Ibuprofen | inhibit | photosensitivity | Cyclooxygenase | angiogenesis | microtubule | breast cancer | Apoptosis | (±)-Ibuprofen | T cells | Neuroprotection | COX | anti-tumor | inflammation | anti-cancer | cystic fibrosis | tumor microenvironment | Ibuprofe | Inhibitor

相关产品: Bromfenac Sodium | Zileuton | Lobuprofen | Dehydroglyasperin D | Paradol | SC-560 | Firocoxib | 2,5-Di-tert-butylhydroquinone | (±)-Catechin | Metyrosine

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Endoplasmic Reticulum Stress Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Nonsteroidal Anti-Inflammatory Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途