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编 号:F444686
分子式:C15H13NO3
分子量:255.27
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50mg
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100mg
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生物活性:
Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research.

体内研究:
Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits.Ketorolac (4 mg/kg/day, p.o.; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats.Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats.Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice.Animal Model:New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation
Dosage:50 μL ketorolac tromethamine ophthalmic solution 0.4%
Administration:In eyes, twice, 2 hours and 1 hour before LPS challenge
Result:Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE2 concentrations in the aqueous humor.
Animal Model:Male Wistar rats (400–450 g), spinal cord ischemia model
Dosage:30 and 60 μg
Administration:Intrathecal injection, 1 h before the ischemia induction for once
Result:Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Animal Model:Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Dosage:20 mg/kg and 30 mg/kg
Administration:IP injection, two times in a week for 3 weeks
Result:Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).

体外研究:
Ketorolac (RS37619) salt (0-30 μM; 48 h) effectively kills the oral cancer cells.Ketorolac salt (0-5 μM; 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells.Ketorolac salt (0-2.5 μM; 0-16 h) inhibits the proliferation of oral cancer cells.Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity.
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