Loxoprofen 是一种具有口服活性和解热作用的非甾体类抗炎药，可用于缓解疼痛的研究。Loxoprofen 是一种非选择性COX抑制剂，对 COX-1 和 COX-2 的IC50分别为 6.5 和 13.5 μM。Loxoprofen 可降低动脉粥样硬化，并具有抗肿瘤活性。
| 生物活性 | Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselectiveCOXinhibitor withIC50s of 6.5 and 13.5 μM forCOX-1andCOX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity[1][2][3][4]. |
| IC50& Target[1] | COX-1 6.5 μM (IC50, in human whole blood) | COX-2 13.5 μM (IC50, in human whole blood) |
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体外研究
(In Vitro) | Loxoprofen, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2 in human whole blood assays, respectively[1].
Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the reasearch of pain and inflammation caused by chronic and transitory conditions. Its alcoholic metabolites are formed by carbonyl reductase (CR) and they consist of trans-LOX, which is active, and cis-LOX, which is inactive. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP)[2].
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体内研究
(In Vivo) | Loxoprofen sodium (4 mg/kg/day; p.o.; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation[3].
Loxoprofen sodium (60 μg/mL; p.o.; 24 days) suppresses mouse tumor growth by inhibiting VEGF[4].
| Animal Model: | ApoE-/-mice (C57BL/6J-Apoetm1Unc) with high-fat diet (0.2% cholesterol, 21% saturated fat) from 8 to 16 weeks of age[3] | | Dosage: | 4 mg/kg/day in drinking water | | Administration: | Oral dosing from 8 to 16 weeks of age or from 15 to 16 weeks of age | | Result: | Inhibited platelet thromboxane production and platelet aggregation. Reduced extent of atherosclerosis. Suppressed the production of PGE2, TxB2and PGI2. |
| Animal Model: | 6-week-old male C57BL/6 and BDF1 mice, 100 μL suspensions (2 × 106cells/mL) of LLC cells and KLN205 cells were injected subcutaneously into C57BL/6 and BDF1 mice, respectively[4]. | | Dosage: | 60 μg/mL | | Administration: | Oral dosing in drinking water, every day for 24 days | | Result: | Suppressed tumor growth and angiogenesis, suppressed expression of VEGF in mice with LLC tumor, inhibited tubular formation of HUVECs. |
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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(406.01 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.0601 mL | 20.3004 mL | 40.6009 mL | | 5 mM | 0.8120 mL | 4.0601 mL | 8.1202 mL | | 10 mM | 0.4060 mL | 2.0300 mL | 4.0601 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 (10.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.15 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 (10.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.15 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 (10.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.15 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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