Home Neuronal Signaling COX inhibitor Naproxen Sodium For research use only.

Naproxen Sodium

Synonyms: RS-3650

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.

Naproxen Sodium Chemical Structure

Naproxen Sodium Chemical Structure

CAS: 26159-34-2

Selleck's Naproxen Sodium has been cited by 2 publications

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Batch: Purity: 100%
100

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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
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]
Kinase Assay 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 PGF2α for the assessment of IC50 for COX-1 and COX-2.
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 2.5, 10 or 25 mg/kg
Administration Intravenously (i.v.) infusion or intraperitoneal (i.p.) injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05900336 Not yet recruiting Dysmenorrhea|Menstrual Pain|Non-steroidal Anti-inflammatory Drug Mclean Hospital|United States Department of Defense|NorthShore University HealthSystem January 1 2024 Phase 4
NCT05844995 Recruiting Orthodontic Pain Johnson & Johnson Consumer Inc. (J&JCI)|Johnson & Johnson Consumer and Personal Products Worldwide September 13 2023 Phase 1
NCT05411718 Recruiting T Cells|Colorectal Cancer|Lynch Syndrome M.D. Anderson Cancer Center|National Institutes of Health (NIH)|National Cancer Institute (NCI) March 21 2023 Phase 2
NCT05026320 Completed Soft Tissue Injury Bayer|Deutsche Sporthochschule Köln August 8 2021 Phase 2

Chemical lnformation & Solubility

Molecular Weight 252.24 Formula

C14H13NaO3
CAS No. 26159-34-2 SDF Download Naproxen Sodium SDF
Smiles CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

Water : 76 mg/mL

Ethanol : 15 mg/mL

DMSO : 3 mg/mL ( (11.89 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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