Ketoprofen (RP-19583) 是一种非甾体抗炎剂，可抑制 cyclooxygenase 的活性，其IC50值为 2 nM (COX-1) 和 26 nM (COX-2)。Ketoprofen 可用于炎症、免疫学和代谢性疾病 (如肥胖) 的相关研究。
| 生物活性 | Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity ofcyclooxygenasewithIC50values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, andmetabolic diseasesuch as obesity[1][2][3]. |
| IC50& Target[1] | COX-1 2 nM (IC50, in human blood monocytes) | COX-2 26 nM (IC50, in human blood monocytes) |
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体外研究
(In Vitro) | Ketoprofen inhibits COX in LPS-stimulated monocytes isolated from human blood, with IC50values of 2 nM (COX-1) and 26 nM (COX-2)[1].Ketoprofen (2.5 mg /mL, 3-24h) decreases the mRNA level of immune factors (TNFα, IL-8, SAA and COX-2) and PTGES in LPS-stimulated bovine mammary epithelial cells[3].
RT-PCR[3] | Cell Line: | LPS (0.2 μg/mL)-stimulated bovine mammary epithelial cells | | Concentration: | 2.5 mg /mL | | Incubation Time: | 3, 6, 24 h | | Result: | Decreased the mRNA level of TNFα, IL-8, SAA, COX-2 and PTGES. |
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体内研究
(In Vivo) | Ketoprofen (Oral administration, 10 mg/kg, three times a week for 10 weeks, HFD-induced obese C57BL/6 mice) decreases in relative body weight (15.41%), the iWAT mass (approximately 41%), and leptin (58.68%) and resistin (12.88%)[2].Ketoprofen (50 mg/kg, LPS-treated dairy cows) lowers the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk induced by LPS[3].
| Animal Model: | HFD-induced obese C57BL/6 mice[2] | | Dosage: | 10 mg/kg | | Administration: | Oral administration, three times a week for 10 weeks | | Result: | Decreased in relative body weight, the iWAT mass, and the level of leptin and resistin. |
| Animal Model: | LPS (0.2 μg/mL)-treated dairy cows[3] | | Dosage: | 50 mg/kg | | Administration: | Injection (Milk samples were taken every 30 min until 6 and 9 h) | | Result: | Lowered the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk. |
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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(393.27 mM) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.9327 mL | 19.6634 mL | 39.3267 mL | | 5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL | | 10 mM | 0.3933 mL | 1.9663 mL | 3.9327 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 (9.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.83 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 (9.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.83 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 (9.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.83 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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