Nabumetone

Research use only, not for human use.

Nabumetone(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.

Nabumetone(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.(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. (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-PGF1α production in rats. 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.

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.

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-PGF1α production in rats. 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.

BRL 14777

Chromatin/Epigenetic

COX

COX-1| COX-2| MPO

Inflammation/Immunology

——

42924-53-8

228.29

C15H16O2

>98% (HPLC)

Ethanol: 25 mg/mL (109.5 mM); DMSO: 46 mg/mL (201.49 mM)

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

4-(6-methoxynaphthalen-2-yl)butan-2-one

(-20℃)

With Ice Pack

≥ 2 years