Ibuprofen ((±)-Ibuprofen) 是一种口服有效的COX-1选择性抑制剂,IC50值为 13 μM。Ibuprofen 抑制细胞增殖、血管生成,并诱导细胞凋亡 (apoptosis)。Ibuprofen 是一种非甾体抗炎试剂和一氧化氮 (NO) 供体。Ibuprofen可用于疼痛、肿胀、炎症、感染、免疫学、癌症的研究。
生物活性 | Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selectiveCOX-1inhibitor with anIC50value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cellapoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation,infection, immunology, cancers[1][2][5][8]. |
IC50& Target[1] | COX-1 13 μM (IC50) | COX-2 370 μM (IC50) |
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体外研究 (In Vitro) | Ibuprofen (24 h) inhibits COX-1 and COX-2 activity with IC50values of 13 μM and 370 μM[1]. Ibuprofen (500 μM, 48 h) inhibits cell proliferation and angiogenesis, and induces apoptosis in AGS cells (Adenocarcinoma gastric cell line)[2]. Ibuprofen (500 μM, 48 h) downregulates transcription of Akt, VEGF-A, PCNA, Bcl2, OCT3/4 and CD44 genes, but upregulates RNA levels of wild type P53 and Bax genes in AGS cell[2]. Ibuprofen (500 μM, 24 h) restores microtubule reformation, microtubule-dependent intracellular cholesterol transport, and induces extension of microtubules to the cell periphery in both cystic fibrosis (CF) cell models and primary CF nasal epithelial cells[3]. Ibuprofen (500 μM, 24 h) enhances UV-induced cell death in MCF-7 cells and MDA-MB-231 cells by a photosensitization process[4].
Cell Viability Assay[2] Cell Line: | AGS cells | Concentration: | 100-1000 μM | Incubation Time: | 24 h, 48 h | Result: | Inhibited AGS cell viability with IC50values of 630 μM (trypan blue staining, 24 h), 456 μM (neutral red assay, 24 h), 549 μM (trypan blue staining, 48 h) and 408 μM (neutral red assay, 48 h). |
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体内研究 (In Vivo) | Ibuprofen (300 mg/kg; p.o.; daily, for 14 days) reduces overall tumor growth and enhances anti-tumor immune characteristics without adverse autoimmune reactions in a model of postpartum breast cancer[5]. Ibuprofen (60 mg/kg; i.h.; every second day for 15 days) reduces the risk of neuropathy in a rat model of chronic Oxaliplatin-induced peripheral neuropathy[6]. Ibuprofen (20 mg/kg; p.o.; every 12 hours, 5 doses total) decreases muscle growth (average muscle fiber cross-sectional area) without affecting regulation of supraspinatus tendon adaptions to exercise[7]. Ibuprofen (35 mg/kg; p.o.; twice daily) attenuates the Inflammatory response topseudomonas aeruginosain a rat model of chronic pulmonary infection[8].
Animal Model: | Syngeneic (D2A1) orthotopic Balb/c mouse model of PPBC (postpartum)[5] | Dosage: | 300 mg/kg, daily for 14 days | Administration: | Fed in animal feedings (added to pulverized standard chow and mixed dry, then mixed with water, made into chow pellets and dried thoroughly) | Result: | Suppresed tumor growth, reduced presence of immature monocytes and increased numbers of T cells. Enhanced Th1 associated cytokines as well as promoted tumor border accumulation of T cells. |
Animal Model: | Oxaliplatin-induced peripheral neuropathy[6] | Dosage: | 60 mg/kg, every second day for 15 days | Administration: | Subcutaneous injection | Result: | Lowered sensory nerve conduction velocity (SNCV). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(484.78 mM;Need ultrasonic) H2O : 1 mg/mL(4.85 mM;Need ultrasonic) 配制储备液 1 mM | 4.8478 mL | 24.2389 mL | 48.4778 mL | 5 mM | 0.9696 mL | 4.8478 mL | 9.6956 mL | 10 mM | 0.4848 mL | 2.4239 mL | 4.8478 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.12 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.12 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.12 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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