Ketoprofen 是一种非甾体抗炎剂，能够有效地抑制COX的活性，在人血单核细胞中，对 COX-1 和 COX-2 的IC50值分别为 2 nM 和 26 nM。

Ketoprofen is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic effects. Ketoprofen inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis, by prostaglandin synthase, is responsible for the therapeutic effects of ibuprofen. Ketoprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.

Ketoprofen combined with UVB irradiation induces the cytotoxicity and suppresses DNA synthesis in HaCaT cells in a concentration-dependent manner. Ketoprofen combined with UVB irradiation inhibits the cell growth and induces G2/M cell cycle arrest by modulating the levels of cdc2, cyclin B1, Chk1, Tyr15-phosphorylated cdc2 and p21. Ketoprofen combined with UVB irradiation also provokes a striking accumulation of cyclin B1-cdc2-p21 complexes, concomitantly with an increase in the levels of Tyr15-phosphorylated cdc2 and p21 protein. Ketoprofen combined with UVB irradiation accentuates the apoptotic response to UVB radiation in HaCaT cells as evidenced by DAPI staining. [1]

Ketoprofen at 1% level in suitable topical vehicles can effectively inhibit GCF-LTB4 and GCF-PGE2 and positively alter alveolar bone activity in the ligature-induced model of periodontitis in the monkey. [2] Ketoprofen (3.63 mg/kg bwt) reduces hoof pain andlameness to a greater extent than the 2.2 mg/kg dose and phenylbutazone. [3] Ketoprofen is more effective than local anesthesia (LA), or caudal epidural anesthesia (EPI) in decreasing cortisol and partially reverses the reduction in average daily gain (ADG) following castration. [4] Ketoprofen (40 and 80 mg/kg diet) reduces the incidence of transitional cell carcinoma of the urinary bladder by >70% from that seen in dietary mice. [5]

22071-15-4

C16H14O3

254.285

RP-19583;酮基布洛芬;酮洛芬

DMSO:48 mg/mL (188.8 mM)
Ethanol:48 mg/mL (188.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years