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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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+ |
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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。 |
靶点 |
|
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]. |
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. |
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 | - | - | |
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 |
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 |