1. Immunology/Inflammation
  2. COX
  3. Nabumetone

Nabumetone (Synonyms: BRL14777)

Cat. No.: HY-B0559 Purity: 99.86%
Handling Instructions

Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.

For research use only. We do not sell to patients.

Nabumetone Chemical Structure

Nabumetone Chemical Structure

CAS No. : 42924-53-8

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Description

Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.

IC50 & Target

COX-2

 

In Vitro

Nabumetone is a potent and selective COX-2 inhibitor. Nabumetone (50 μmol-2 mmol) dose-dependently inhibits the proliferation of K-562 and Meg-01 cells, but shows no obvious apoptotic effect. Nabumetone potentiates the apoptotic effect of ADR in the K-562 cell line. Moreover, Nabumetone reduces Bcl-2 expression[1].

In Vivo

Nabumetone (79 mg/kg, p.o.) inhibits paw oedema and paw exudate PGE2 in rats. Nabumetone does not induce gastric damage and causes only 57% inhibition of gastric mucosal 6-keto-PGF production in rats[2]. Nabumetone (25, 50, 100 mg/kg, i.p.) dose-dependently inhibits the increase of DDC-induced mucus secretion and stimulates stress-induced mucus secretion in rats. Nabumetone (25 mg/kg, i.p.) significantly suppresses stress-induced ulcer index in rats[3].

Clinical Trial
Molecular Weight

228.29

Formula

C₁₅H₁₆O₂

CAS No.

42924-53-8

SMILES

CC(CCC1=CC=C2C=C(OC)C=CC2=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (438.04 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3804 mL 21.9020 mL 43.8039 mL
5 mM 0.8761 mL 4.3804 mL 8.7608 mL
10 mM 0.4380 mL 2.1902 mL 4.3804 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Every cell line is plated into 6-well plates at a concentration of 3 × 105/mL with or without drugs (Nabumetone, etc.) and incubated for 48 h. Viable cells are then counted using the trypan blue dye exclusion test. The percentage of proliferation inhibition is calculated as 1-(viable cells exposed to drug/viable cells in control) ×100[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Rats[3]
Albino male rats (250- to 300-g body weight) are used in the study. The animals are maintained in a single cage and are deprived of food for 16 h before the onset of experiments. Free access to water is allowed until 1 h before the beginning of experiments. There are eight rats in each group. The animals are pretreated with intraperitoneal injections of Nabumetone or dipyrone at 25-, 50-, or 100-mg/kg doses for 3 days[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.86%

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Keywords:

NabumetoneBRL14777BRL 14777BRL-14777COXCyclooxygenaseInhibitorinhibitorinhibit

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