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KI0711Phenylbutazone50 mg$154

Chemical Characteristic

Product NamePhenylbutazone
SynonymsButazolidin, Azolid
CAS No.50-33-9
Molecular Weight 308.37
FormulaC19H20N2O2
Chemical Structure

Biological activities

Phenylbutazone is a nonsteroidal anti-inflammatory drug (NSAID) for the short-term treatment of pain and fever in animals. In vitro, phenylbutazone significantly increases the plasma protein binding of aurothiomalate.[1] The IC50 of phenylbutazone for inhibition of salvianolic acid A glucuronidation is 50.3 and 39.4 µM by HLMs and UGT1A9, respectively.[2] Phenylbutazone inhibits both oxidative and substrate-level phosphorylations. Phenylbutazone inhibits the generation of energy-rich phosphate compounds (ATP, acetyl phosphate) by suppressing respiration at multiple sites. [3] Phenylbutazone (5 mM) inhibits incorporation of [1-14C] glucosamine and [14C] leucine into acid precipitable protein by rat intestinal slices. Phenylbutazone inhibits [1-14C] glucosamine incorporation by cycloheximide-treated slices. [4] Phenylbutazone inhibits epithelial cell death in vivo. [5]

References

[1] Mason RW. The binding of aurothiomalate to plasma proteins in vitro. Pharmacology. 1977, 15(6): 536-544. 閵嗏偓閵嗏偓
[2] Han DE, et al. Identification and characterization of human UDP-glucurono- syltransferases responsible for the in vitro glucuronidation of salvianolic acid A. Drug Metab Pharmacokinet. 2012, 27(6): 579-585. 閵嗏偓閵嗏偓
[3] Tokumitsu Y, et al. In vitro effects of nonsteroidal anti-inflammatory drugs on oxidative phosphorylation in rats liver mitochondria. Biochem Pharmacol. 1977, 26 (22): 2101-2106 閵嗏偓閵嗏偓
[4] Lukie BE, et al. Synthesis of intestinal glycoproteins inhibitions of [1-14C] glucosamine incorporation by phenylbutazone in vitro. Biochimica et Biophysica Acta (BBA) - General Subjects. 1974, 338(2): 345-351. 閵嗏偓閵嗏偓
[5] Montenegro MA, et al. Light and electron microscopic study on the effect of phenylbutazone on developing mouse palatal epithelium in vitro. Arch Oral Biol. 1982, 27 (9): 771-775. 閵嗏偓

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