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酮洛芬 /Ketoprofen {[allProObj[0].p_purity_real_show]}

货号:A164797 同义名: 酮基布洛芬 / RP-19583;2-(3-benzoylphenyl)Propionic Acid

Ketoprofen is a dual COX1/2 inhibitor with IC50 of 0.5 μM and 2.33 μM for human recombinant COX-1 and COX-2, respectively, and used as a nonsteroidal anti-inflammatory drug (NSAID) to treat arthritis-related inflammatory pains.

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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+
Ketoprofen 化学结构 CAS号:22071-15-4
Ketoprofen 化学结构
CAS号:22071-15-4
Ketoprofen 3D分子结构
CAS号:22071-15-4
Ketoprofen 化学结构 CAS号:22071-15-4
Ketoprofen 3D分子结构 CAS号:22071-15-4
规格 价格 会员价 库存 数量
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Ketoprofen 纯度/质量文件 产品仅供科研

货号:A164797 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 99%
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%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
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

98%
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。

Ketoprofen 生物活性

靶点
  • COX-1

描述 Cyclooxygenase (COX) is the rate-limiting enzyme for the synthesis of prostaglandins. Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits both COX1 and COX2 in blood with the IC50 values of 0.11 μM and 0.88 μM, respectively[1]. Ketoprofen inhibited thromboxane B2 (TxB2) production in freshly isolated platelets from human blood with an IC50 value of 7.4 μM. The efficacy of ketoprofen in inhibiting LPS-induced TxB2 production in human mononuclear cells was determined with an IC50 value of 7.7 μM[2]. When HaCaT cells were irradiated with UVB (10 mJ/cm2), the activity of caspase-3 and the number of cells at the G2 phase were significant increased compared to cells without ketoprofen treatment. It was also shown that 100 μM Ketoprofen significantly provoked the accumulation of cyclin B1-cdc2-p21 complexes, as well as the amounts of Tyr15-phosphorylated cdc2 and p21 protein[3].
作用机制 Ketoprofen inhibits the activity of cyclooxygenase by conjugating with glucuronide and with coenzyme A[4].

Ketoprofen 动物研究

Dose Dog: 0.5 mg/kg - 2 mg/kg[5] (s.c.); 0.25 mg/kg - 5 mg/kg[5] (p.o.) Rat: 50 mg/kg[6] (p.o.)
Administration s.c., p.o.

Ketoprofen 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01307020 Pain Phase 2 Completed - Germany ... 展开 >> Klinik und Polickinik für Mund-Kiefer-Gesichtschirurgie/Plastische Operationen Greifswald Greifswald, Mecklenburg-Vorpommern, Germany, 17475 Klinik für Mund-, Kiefer- und Gesichtschirurgie, Universitätsklinikum Schleswig Holstein, Campus Kiel Kiel, Schleswig-Holstein, Germany, 24105 Hungary Dr Tóth Bagi Zoltán Fogászati Rendeloje Budapest, Hungary, 1052 Italy Centro di Farmacologia Clinica per la Sperimentazione dei Farmaci Pisa, Italy, 56126 Centro di Ricerche Cliniche di Verona Srl. Policlinico G.B.Rossi Verona, Italy, 37134 Poland Gabinet Stomatologiczny Andrzej Wojtowicz AW Clinic Warsaw, Mazowieckie, Poland, 00-852 Dental Service spólka jawna Warszawa, Mazowieckie, Poland, 02-791 Spain Hospital Médico Quirúrgico de Conxo Santiago de Compostela, A Coruña, Spain, 15706 Facultad de Odontología. Departamento de Cirugía Bucal y Maxilofacial, University of Barcelona - Bellvitge Institute for Biomedical Research (IDIBELL) L'Hospitalet de Llobregat, Barcelona, Spain, 08907 Universidad Complutense de Madrid Madrid, Spain, 28040 Departamento de Estomatología, Facultad de Odontología. Universidad de Sevilla Sevilla, Spain, 41009 Departament d'Estomatologia, Clínica Odontològica, Universidad de Valencia - Fundació Lluís Alcanyís Valencia, Spain, 046010 Hospital General Universitario de Valencia Valencia, Spain, 46014 United Kingdom The School of Dentistry, College of Medical and Dental Sciences, University of Birmingham Birmingham, England, United Kingdom, B4 6 NN University Dental School Manchester Manchester, England, United Kingdom, M15 6FH University Dental Hospital Cardiff, Wales, United Kingdom, CF14 4 XY 收起 <<
NCT02092012 Pain Phase 4 Unknown July 2014 Turkey ... 展开 >> Erciyes Univercity Medicine Faculty Recruiting Kayseri, Turkey, 38039 Contact: selda kayaaltı, resident    +905558168918    drselda@hotmail.com    Contact: fatih ugur, assoc    +905359730073    ugurf@erciyes.edu.tr 收起 <<
NCT01307020 - Completed - -

Ketoprofen 参考文献

[1]Cryer B, Feldman M. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med. 1998;104(5):413-21.

[2]Grossman CJ, Wiseman J, et al. Inhibition of constitutive and inducible cyclooxygenase activity in human platelets and mononuclear cells by NSAIDs and Cox 2 inhibitors. Inflamm Res. 1995;44(6):253-7.

[3]Liu S, Mizu H, et al. Molecular response to phototoxic stress of UVB-irradiated ketoprofen through arresting cell cycle in G2/M phase and inducing apoptosis. Biochem Biophys Res Commun. 2007;364(3):650-5.

[4]Levoin N, Blondeau C, et al. Elucidation of the mechanism of inhibition of cyclooxygenases by acyl-coenzyme A and acylglucuronic conjugates of ketoprofen. Biochem Pharmacol. 2004;68(10):1957-69.

Ketoprofen 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.66mL

3.93mL

1.97mL

39.33mL

7.87mL

3.93mL

Ketoprofen 技术信息

CAS号22071-15-4
分子式C16H14O3
分子量 254.28
别名 酮基布洛芬 ;RP-19583;2-(3-benzoylphenyl)Propionic Acid;(R,S)-Ketoprofen;(±)-Ketoprofen
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(412.93 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
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