| Identification | Back Directory | [Name]
LOXOPROFEN SODIUM SALT | [CAS]
226721-96-6 | [Synonyms]
LOXOPROFEN SODIUM SALT
Loxoprofen SodiuM Salt Dihydrate
LoxoprofenSodiumSaltDihydrate>
2-[4-[(2-Oxocyclopentyl)methyl]phenyl]propionic Acid Sodium Salt | [Molecular Formula]
C15H17NaO3.2H2O | [MDL Number]
MFCD01745788 | [MOL File]
226721-96-6.mol | [Molecular Weight]
304.314 |
| Chemical Properties | Back Directory | [Melting point ]
198°C(dec.)(lit.) | [solubility ]
Methanol (Sparingly), Water (Slightly) | [form ]
powder to crystal | [color ]
White to Almost white | [Merck ]
14,5589 | [Stability:]
Hygroscopic | [CAS DataBase Reference]
226721-96-6 |
| Safety Data | Back Directory | [RIDADR ]
UN 2811 6.1/PG III | [RTECS ]
CY1678845 | [HS Code ]
2918.30.3000 | [HazardClass ]
6.1 | [PackingGroup ]
III |
| Hazard Information | Back Directory | [Uses]
Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity[1][2][3][4]. | [Definition]
ChEBI: Loxoprofen sodium hydrate is a hydrate that is the dihydrate form of loxoprofen sodium. The parent acid, loxoprofen, is a prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor and an antipyretic. It contains a loxoprofen sodium. | [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, TxB2 and PGI2.
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| 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[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. |
| [IC 50]
COX-1: 6.5 μM (IC50, in human whole blood); COX-2: 13.5 μM (IC50, in human whole blood) | [References]
[1] Riendeau D, et al. Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004;14(5):1201-1203. DOI:10.1016/j.bmcl.2003.12.047
[2] Paudel S, et al. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9):479. Published 2019 Sep 16. DOI:10.3390/pharmaceutics11090479
[3] Hamaguchi M, et al. Loxoprofen Sodium, a Non-Selective NSAID, Reduces Atherosclerosis in Mice by Reducing Inflammation. J Clin Biochem Nutr. 2010 Sep;47(2):138-47. DOI:10.3164/jcbn.10-33
[4] Kanda A, et al. Loxoprofen sodium suppresses mouse tumor growth by inhibiting vascular endothelial growth factor. Acta Oncol. 2003;42(1):62-70. DOI:10.1080/0891060310002258 |
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TCI Europe
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320-37350700 |
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https://www.tcichemicals.com/de/de/index.html |
| Company Name: |
TCI AMERICA
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| Tel: |
800-4238616 |
| Website: |
https://www.tcichemicals.com/en/us/index.html |
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