(S)-(+)-Ibuprofen ((S)-Ibuprofen),一种 Ibuprofen 的 S(+)-对映异构体,是一种有效的COX-1和COX-2抑制剂,IC50分别为 2.1μM 和 1.6 μM。(S)-(+)-Ibuprofen 具有止痛,抗炎,抗癌和退热作用。
生物活性 | (S)-(+)-Ibuprofen ((S)-Ibuprofen), a S(+)-enantiomer of Ibuprofen, is a potentCOX-1andCOX-2inhibitor withIC50s of 2.1 μM and 1.6 μM, respectively. (S)-(+)-Ibuprofen has analgesic, anti-inflammatory, anticancer and antipyretic effects[1][2]. |
IC50& Target[1] | COX-1 2.1 μM (IC50) | COX-2 1.6 μM (IC50) |
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体外研究 (In Vitro) | (S)-(+)-Ibuprofen (HCT-15 and HCA-7 cells; 0-1000 μM; 8 days) treatment reduces concentration dependently cell survival in both cell lines to a similar extent[2]. (S)-(+)-Ibuprofen (HCT-15 and HCA-7 cells; 0-1000 μM; 20-72 hours) treatment causes a G0/G1 phase block as well as apoptosis[2]. (S)-(+)-Ibuprofen (HCT-15 and HCA-7 cells; 900 μM; 4-72 hours) treatment shows a down regulation of cyclin A and B and an increase of the cell cycle inhibitory protein p27Kip-1[2]. (S)-(+)-Ibuprofen inhibits COX activity, thromboxane formation, and platelet aggregation[1]. (S)-(+)-Ibuprofen inhibits the activation of NF-κB in response to T-cell stimulation with an IC50of 61.7 μM[3].
Cell Proliferation Assay[2] Cell Line: | HCT-15 and HCA-7 cells | Concentration: | 0 μM, 200 μM, 400 μM, 600 μM, 700 μM, 800 μM, 900 μM, and 1000 μM | Incubation Time: | 8 days | Result: | Reduced concentration dependently cell survival in both cell lines to a similar extent. |
Cell Cycle Analysis[2] Cell Line: | HCT-15 and HCA-7 cells | Concentration: | 0 μM, 200 μM, 400 μM, 600 μM, 800 μM, 900 μM, and 1000 μM | Incubation Time: | 24 hours (HCT-15) or 20 hours (HCA-7) | Result: | Caused a G0/G1 phase block. |
Apoptosis Analysis[2] Cell Line: | HCT-15 and HCA-7 cells | Concentration: | 0 μM, 200 μM, 400 μM, 600 μM, 800 μM, 900 μM, and 1000 μM | Incubation Time: | 72 hours | Result: | Induced cell apoptosis. |
Western Blot Analysis[2] Cell Line: | HCT-15 and HCA-7 cells | Concentration: | 900 μM | Incubation Time: | 4 hours, 8 hours, 16 hours, 24 hours, 32 hours, 48 hours and 72 hours | Result: | Decreased levels of Cyclin D1 protein. |
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体内研究 (In Vivo) | (S)-(+)-Ibuprofen (15 mg/kg/day; intraperitoneal injection; five days a week; for 4 weeks) treatment inhibits tumor growth of HCA-7 and HCT-15 xenografts in the nude mice model[2].
Animal Model: | NMRI (nu/nu) male mice (6-8 week old ) injected with HCA-7 and HCT-15 cells[2] | Dosage: | 15 mg/kg/day | Administration: | Intraperitoneal injection; five days a week; for 4 weeks | Result: | Inhibited tumor growth of HCA-7 and HCT-15 xenografts in mice. |
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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) Ethanol : 100 mg/mL(484.78 mM;Need ultrasonic) H2O : 1 mg/mL(4.85 mM;Need ultrasonic and warming) 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: PBS Solubility: 6.67 mg/mL (32.33 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 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。 3. 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。 4. 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。 5. 请依序添加每种溶剂: 10% EtOH 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 EtOH 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 6. 请依序添加每种溶剂: 10% EtOH 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 EtOH 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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