Ketorolac (RS37619) 是一种非甾体抗炎剂，为非选择性的COX抑制剂，对 COX-1 和 COX-2 的IC50值分别为 20 nM 和 120 nM。Ketorolac被用作 0.5% 滴眼液，用于过敏性结膜炎、黄斑囊状水肿、术中瞳孔缩小、术后眼炎疼痛的研究。Ketorolac 也是一种DDX3抑制剂，可用于癌症的研究。
| 生物活性 | Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselectiveCOXinhibitor, withIC50s of 20 nM forCOX-1and 120 nM forCOX-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 aDDX3inhibitor that can be used forcancerresearch[1][4]. |
| IC50& Target[1] | COX-1 20 nM (IC50) | COX-2 120 nM (IC50) | DDX3 |
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体外研究
(In Vitro) | Ketorolac (RS37619) salt (0-30 μM; 48 h) effectively kills the oral cancer cells[4].
Ketorolac salt (0-5 μM; 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells[4].
Ketorolac salt (0-2.5 μM; 0-16 h) inhibits the proliferation of oral cancer cells[4].
Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity[4].
Cell Viability Assay[4] | Cell Line: | HOK, SCC4, SCC9 and H357 cells | | Concentration: | 0-30 μM | | Incubation Time: | 48 h | | Result: | Showed inhibition with IC50s of 2.6, 7.1 and 8.1 μM against H357, SCC4 and SCC9 cells, respectively. And the normal HOK cell line did not show any cell death effect. |
Cell Proliferation Assay[4] | Cell Line: | H357 | | Concentration: | 0.5, 1.0, 1.5, 2.0 and 2.5 μM | | Incubation Time: | 0, 8 and 16 h | | Result: | Inhibited the proliferation. |
Western Blot Analysis[4] | Cell Line: | H357 | | Concentration: | 1, 2.5 and 5 μM | | Incubation Time: | 48 h | | Result: | Significantly reduced DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin. |
Apoptosis Analysis[4] | Cell Line: | H357 | | Concentration: | 2.5 and 5 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis. |
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体内研究
(In Vivo) | Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits[1].
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[2].
Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats[3].
Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice[4].
| Animal Model: | New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation[1] | | 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 PGE2concentrations in the aqueous humor. |
| Animal Model: | Male Wistar rats (400–450 g), spinal cord ischemia model[3] | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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