Loxoprofen

SKU: orb1224242

Description

Loxoprofen is a non-steroidal anti-inflammatory drug.(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.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).(In Vivo):Loxoprofen sodium (4 mg/kg/day; p.o.; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation. Loxoprofen sodium (60 μg/mL; p.o.; 24 days) suppresses mouse tumor growth by inhibiting VEGF.

Key Properties

• CAS Number: 68767-14-6
• MW: 246.3
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₈O₃
• SMILES: CC(C(O)=O)C1=CC=C(CC2CCCC2=O)C=C1
• Target: COX
• Solubility: Soluble in DMSO

Bioactivity

• In Vivo:
  Loxoprofen sodium (4 mg/kg/day; p.o. ; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation. Loxoprofen sodium (60 μg/mL; p.o. ; 24 days) suppresses mouse tumor growth by inhibiting VEGF. Animal model: ApoE-/-mice (C57BL/6J-Apoetm1Unc) with high-fat diet (0.2% cholesterol, 21% saturated fat) from 8 to 16 weeks of age. 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, TxB2 and PGI2. Animal model: 6-week-old male C57BL/6 and BDF1 mice, 100 μL suspensions (2 × 106 cells/mL) of LLC cells and KLN205 cells were injected subcutaneously into C57BL/6 and BDF1 mice, respectively. 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.
• 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. 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

COX