Ketorolac 是一种非甾体抗炎化合物,作为 COX-1 和 COX-2 的非选择性抑制剂(IC50 分别为 1.23 μM 和 3.50 μM),常用于过敏性结膜炎、黄斑囊状水肿及术后眼炎疼痛的研究。


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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 | ✔ | 98% | |||||||||||||||||
| 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% | ||||||||||||||||
| 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 |
95% | |||||||||||||||||
| 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 | Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. In the animal model, both ketorolac 0.4% and bromfenac 0.09% demonstrated maximal anti-inflammatory activity in treated eyes[3]. Ketorolac (4 mg/kg/day, p.o.) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats[4]. Ketorolac (60 μg/10 μL) reduces the histological changes such as ischemic cell death, including cytoplasmic eosinophilia with disintegration of cytoarchitecture and nuclear pyknosis in rats. Intrathecal pretreatment with 60 microg of ketorolac significantly reduced neuronal death and improved hindlimb motor function, and the long-term survival was similar to that in the control group[5]. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | C26 or CHX207 tumor model | Oral | 2 mg/kg | Daily until study endpoint | R-ketorolac (RK) ameliorated cancer-associated cachexia, prolonged survival of tumour-bearing mice, reduced loss, and improved muscle and adipose tissue loss. | J Cachexia Sarcopenia Muscle. 2024 Apr;15(2):562-574 |
| C57BL/6J mice | Orthotopic pancreatic cancer model | Intraperitoneal injection | 2 mg/kg | Single dose | Ketorolac was used for post-operative analgesia, and its effect on tumor growth was not mentioned. | Cells. 2024 Jun 19;13(12):1061 |
| Mice | LSL-KrasG12D/+;Trp53f/f;Pdx1-Cre mouse model | Intraperitoneal injection | 2 mg/kg | Single injection | Ketorolac was used for post-surgical analgesia, and the experimental results did not mention specific effects. | Cell Rep. 2019 Oct 29;29(5):1287-1298.e6 |
| Mice | Pancreatic cancer model | Intraperitoneal injection | 2 mg/kg | Single dose | Postoperative pain relief | J Clin Invest. 2019 May 21;129(8):3264-3276 |
| Mice | Injury-induced peripheral inflammation model | Subcutaneous injection | 30 mg/kg | Single injection, measured 1 hour later | To evaluate the anti-inflammatory effect of Ketorolac on CFA-induced inflammation, results showed that food deprivation had a larger anti-inflammatory effect than Ketorolac | Cell Rep. 2023 Nov 28;42(11):113338 |
| Mice | C57BL/6NHsd mice | Subcutaneous injection | 5 mg/kg | Immediately after surgery and 24 hours later | Provide postoperative analgesia | Neuropharmacology. 2022 Sep 1;215:109168 |
| Mice | Young and adult mice | Intraperitoneal injection | 1 mg/kg | 30 minutes before each anesthesia, for three days | Ketorolac ameliorated the sevoflurane anesthesia-induced cognitive impairment | Anesthesiology. 2013 Mar;118(3):502-15 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.92mL 0.78mL 0.39mL |
19.59mL 3.92mL 1.96mL |
39.17mL 7.83mL 3.92mL |
|
| CAS号 | 74103-06-3 |
| 分子式 | C15H13NO3 |
| 分子量 | 255.27 |
| SMILES Code | O=C(C1C2=CC=C(C(C3=CC=CC=C3)=O)N2CC1)O |
| MDL No. | MFCD00864281 |
| 别名 | RS37619 |
| 运输 | 蓝冰 |
| InChI Key | OZWKMVRBQXNZKK-UHFFFAOYSA-N |
| Pubchem ID | 3826 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, room temperature |
| 溶解方案 |
DMSO: 250 mg/mL(979.36 mM),配合低频超声助溶,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 |
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