Loxoprofen sodium dihydrate 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 sodium dihydrate 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 sodium dihydrate 可降低动脉粥样硬化，并具有抗肿瘤活性。
| 生物活性 | Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselectiveCOXinhibitor withIC50s of 6.5 and 13.5 μM forCOX-1andCOX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity[1][2][3][4]. |
| IC50& Target | 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 sodium dihydrate, 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) sodium dihydrate 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 sodium dihydrate 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) dihydrate reduces atherosclerosis in mice by reducing inflammation[3].
Loxoprofen sodium (60 μg/mL; p.o.; 24 days) dihydrate 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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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