产品说明书

Phenylbutazone

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Chemical Structure| 50-33-9 同义名 : 苯基丁氮酮 ;Butazolidine
CAS号 : 50-33-9
货号 : A208133
分子式 : C19H20N2O2
纯度 : 97%
分子量 : 308.37
MDL号 : MFCD00005500
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(340.5 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Phenylbutazone (PB), a nonsteroidal anti-inflammatory drug, is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Prostacyclin synthase is even more sensitive to inactivation by the combined PB and H2O2 treatment, with a corresponding half-maximal effect at PB concentrations near 25 mM[3]. However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50[4]. Phenylbutazone acts by inhibiting the cyclooxygenase enzyme system, which is responsible for synthesis of prostanoids such as PGE2. It markedly reduces prostanoid-dependent swelling, edema, erythema, and hypersensitivity to pain in inflamed tissues. Phenylbutazone is highly bound (greater than 98%) to plasma protein. After i.v. injection, blood levels decline with an elimination half-life of 3-10 h. The plasma kinetics of phenylbutazone may be dose dependent, with the plasma half-life increasing as the drug dosage level increases. Plasma residues of the drug at 24 h after a single i.v. dose of 2g/450 kg average about 0.9 mg/ml, but considerable variation occurs. Under optimal conditions, the bioavailability of oral phenylbutazone is probably in the region of 70%[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.21mL

3.24mL

1.62mL

32.43mL

6.49mL

3.24mL

参考文献

[1]Zhou J, Li X, . Phenylbutazone, a New Long-Acting Agent that can Improve the Peptide Pharmacokinetic Based on Serum Albumin as a Drug Carrier. Chem Biol Drug Des. 2016 Jun;87(6):936-45.

[2]de Grauw JC, van Loon JP, et al. In vivo effects of phenylbutazone on inflammation and cartilage-derived biomarkers in equine joints with acute synovitis. Vet J. 2014 Jul;201(1):51-6.

[3]Reed GA, Griffin IO, Eling TE. Inactivation of prostaglandin H synthase and prostacyclin synthase by phenylbutazone. Requirement for peroxidative metabolism. Mol Pharmacol. 1985 Jan;27(1):109-14

[4]Beretta C, Garavaglia G, Cavalli M. COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis. Pharmacol Res. 2005 Oct;52(4):302-6

[5]Tobin T, Chay S, Kamerling S, Woods WE, Weckman TJ, Blake JW, Lees P. Phenylbutazone in the horse: a review. J Vet Pharmacol Ther. 1986 Mar;9(1):1-25