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Phenylbutazone/保泰松 {[allProObj[0].p_purity_real_show]}

货号:A208133 同义名: 苯基丁氮酮 / Butazolidine

Phenylbutazone 是一种非甾体抗炎化合物,常用于慢性疼痛(包括关节炎症状)的研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Phenylbutazone/保泰松 化学结构 CAS号:50-33-9
Phenylbutazone/保泰松 化学结构
CAS号:50-33-9
Phenylbutazone/保泰松 3D分子结构
CAS号:50-33-9
Phenylbutazone/保泰松 化学结构 CAS号:50-33-9
Phenylbutazone/保泰松 3D分子结构 CAS号:50-33-9
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Phenylbutazone/保泰松 纯度/质量文件 产品仅供科研

货号:A208133 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 98%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

98%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Phenylbutazone/保泰松 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].

Phenylbutazone/保泰松 细胞实验

Cell Line
Concentration Treated Time Description References
YAMC cells 0.4 mM 24 h To investigate the effect of Phenylbutazone on p62 nuclear translocation in YAMC cells, results showed that Phenylbutazone increased nuclear translocation of p62, indicating potential induction of endoplasmic reticulum stress. Microbiome. 2024 Apr 15;12(1):74.

Phenylbutazone/保泰松 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Horses NSAID-induced intestinal inflammation model Oral 4.4 mg/kg Once daily for 9 days To study the effects of Phenylbutazone on a horse model of intestinal inflammation, results showed that Phenylbutazone induced changes in the microbiota, metabolome, and host transcriptome, correlating with genes and metabolites linked to oxidative stress. Microbiome. 2024 Apr 15;12(1):74.

Phenylbutazone/保泰松 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

Phenylbutazone/保泰松 实验方案

计算器
存储液制备 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

Phenylbutazone/保泰松 技术信息

CAS号50-33-9
分子式C19H20N2O2
分子量 308.37
SMILES Code O=C(C1CCCC)N(C2=CC=CC=C2)N(C3=CC=CC=C3)C1=O
MDL No. MFCD00005500
别名 苯基丁氮酮 ;Butazolidine
运输蓝冰
InChI Key VYMDGNCVAMGZFE-UHFFFAOYSA-N
Pubchem ID 4781
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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