Naproxen Sodium

For research use only.

Catalog No.S1626 Synonyms: RS-3650

2 publications

Naproxen Sodium Chemical Structure

CAS No. 26159-34-2

Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.

Selleck's Naproxen Sodium has been cited by 2 publications

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Biological Activity

Description Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.
Features Displays approximately equipotent inhibitory selectivity for COX-1 and COX-2 in intact cells.
Targets
COX-2 [1] COX-1 [1]
5.2 μM 8.7 μM
In vitro

Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC50 of 2.2 μg/mL and 1.3 μg/mL, respectively. [1] Naproxen decreases the in vitro LPS-induced PGE2 and TXB2 production in rats and humans with IC50 of 30.7 μM and 79.5 μM for PGE2 inhibition, 72.4 μM and 48.3 μM for TXB2 inhibition, respectively. [2] Naproxen produces concentration-related inhibition of TXB2 production from human platelets and LPS-induced TXB2 production from human mononuclear cells with plC50 values (-log concentration inhibiting TXB2 by 50%) of 5.7 and 6.4, respectively, and exhibits slightly inhibitory selectivity for constitutive and induced COX-2 with IC50 COX-1/IC50 COX-2 of 6.3. [3] Only high concentration of Naproxen can significantly induce apoptosis at 48 hours in HCA-7 colon cancer cells with IC50 of 1.45 mM. [4]

In vivo Administration of Naproxen reduces the LPS-induced PGE2 and TXB2 production in vivo in rats with IC50 values of 12.8 μM and 5.9 μM, respectively, which represents that Naproxen is a nonselective COX inhibitor with the log IC50 ratio (COX-2/COX-1) of 0.34. [2] Naproxen displays IC50 of 27 μM for analgesia in a rat model with carrageenan-induced arthritis and IC50 of 40 μM for antipyretics in a yeast-induced fever rat model, while exhibits inhibition of PGE2 with IC50 of 13 μM and TXB2 with IC50 of 5 μM. [5]

Protocol

Kinase Assay:[1]
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COX-1 and COX-2 activities in intact cells:

For the determination of COX-1 and COX-2 inhibition, bovine aortic endothelial cells (BAEC) are incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), and cultured J774.2 macrophages are treated with endotoxin at 1 μg/mL for 12 hours to induce COX-2 followed by incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), respectively. Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 minutes at 37 °C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF1α, PGE2, thromboxane B2, or PGF for the assessment of IC50 for COX-1 and COX-2.
Cell Research:[4]
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  • Cell lines: Human colon cancer HCA-7 cell lines
  • Concentrations: Dissolved in culture medium, final concentration ~20 mM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are exposed to Naproxen for 24 and 48 hours, respectively. At the end of incubation, cells are harvested by trypsinization, stained with trypan blue solution (0.04% wt/vol) and counted in a Neubauer haemocytometer chamber for the determination of cell viability.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 2.5, 10 or 25 mg/kg
  • Administration: Intravenously (i.v.) infusion or intraperitoneal (i.p.) injection
    (Only for Reference)

Solubility (25°C)

In vitro Water 50 mg/mL (198.22 mM)
DMSO 3 mg/mL (11.89 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 252.24
Formula

C14H13NaO3

CAS No. 26159-34-2
Storage powder
in solvent
Synonyms RS-3650
Smiles CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)[O-].[Na+]

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05026320 Recruiting Drug: Naproxen gel|Drug: Diclofenac gel|Drug: Placebo gel Soft Tissue Injury Bayer|Deutsche Sporthochschule Köln August 8 2021 Phase 2
NCT04145518 Recruiting Drug: Naproxen Sodium Dysmenorrhea (Disorder)|Dysmenorrhea Primary|Dysmenorrhea Secondary|Endometrial Diseases|Leiomyoma|Fibroid Uterus NorthShore University HealthSystem|National Institutes of Health (NIH)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) October 25 2019 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID