Home Neuronal Signaling COX inhibitor Nabumetone For research use only.

Nabumetone

Synonyms: BRL-14777

Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.

Nabumetone Chemical Structure

Nabumetone Chemical Structure

CAS No. 42924-53-8

Purity & Quality Control

Nabumetone Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Biological Activity

Description Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.
Features Greater potency than Aspirin.
Targets
COX [1]
In vitro
In vitro Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially COX-2. [1]
In Vivo
In vivo Nabumetone displays acute anti-inflammatory activity in the carrageenan-induced oedema model in rats and the ultraviolet-induced erythema model in guinea-pigs. Its activity in these tests is greater than that of aspirin but less than that of naproxen and indomethacin. In the cotton pellet-induced granuloma model in the rat, Nabumetone is active and produces no signs of toxicity at doses much greater than the lowest effective dose, unlike aspirin, naproxen or indomethacin. Nabumetone is also active in the adjuvant-induced arthritis test in rats. In contrast to aspirin, indomethacin and naproxen, Nabumetone is well tolerated by the stomach of fasted rats at doses in excess of those with anti-inflammatory activity. [2]

Chemical Information & Solubility

Molecular Weight 228.29 Formula

C15H16O2
CAS No. 42924-53-8 SDF --
Smiles CC(=O)CCC1=CC2=C(C=C1)C=C(C=C2)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (201.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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