For research use only.

Catalog No.S1646

2 publications

Ketorolac Chemical Structure

CAS No. 74103-06-3

Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.

Selleck's Ketorolac has been cited by 2 publications

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Biological Activity

Description Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.
Features A COX-1 preferential inhibitor among currently marked nonsteroidal anti-inflammatory drugs (NSAIDs).
COX-1 (human) [1] COX-2 (human) [1]
1.23 μM 3.50 μM
In vitro

(R, S)-, (S)-, and (R)-Ketorolac inhibit both isoforms of COX in recombinant rat and human enzyme systems, and similar as inhibitors of rat COX (rCOX) and human COX (hCOX) under the conditions used. (R, S)-Ketorolac inhibits rat COX-1, rat COX-2, human COX-1 and human COX-2 with IC50 of 0.27 μM, 2.06 μM, 1.23 μM and 3.50 μM, respectively. The (S) enantiomer of Ketorolac with IC50 of 0.10 μM for rat COX-1 is approximately twice as potent as the racemate, whereas the (R)-enantiomer with IC50 of > 100 μM is virtually without activity. [1] Ketorolac shows inhibition of eicosanoid formation in HEL cells (COX-1) and LPS-stimulated Mono Mac 6 cells (COX-2) with IC50 of 0.025 μM and 0.039 μM, respectively, but does not significantly inhibit NO accumulation in supernatants of LPS-stimulated RAW 264.7 cells up to 300 μM. [2] Ketorolac significantly inhibits thymidine incorporation of human osteoblasts (hOBs) upon 24 hours treatment in a dose-dependent manner, and inhibits proliferation and arrests cell cycle at G0/G1 phase in hOBs. [3]

In vivo (R, S)-Ketorolac is significantly more potent than indomethacin or diclofenac sodium in tests of acetic acid-induced writhing, carrageenan-induced paw hyperalgesia, and carrageenan-induced edema formation in rats, with ID50 of 0.24, 0.29 and 0.08 mg/kg, respectively. [1] Ketorolac produces significant inhibition of COX-1 activity and gastric PG synthesis with doses of ≥1 mg/kg inhibiting COX-1 activity by 95% and gastric PG synthesis by >88%. Ketorolac does not significantly affect COX-2 activity at doses of ≤3 mg/kg, but at doses of 10 and 30 mg/kg, Ketorolac produces significant inhibition of COX-2 activity by 75% and 91%, respectively. Ketorolac causes gastric damage in rats only at doses that inhibits both COX-1 and COX-2, or when given with a COX-2 inhibitor. [4]


Kinase Assay:[1]
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Inhibition of Prostaglandin Formation:

Recombinant COX-1 and COX-2 from rat (rCOX) and human (hCOX) expressed in a baculovirus system are purified and reconstituted with 2 mM phenol and 1 μM hematin. Then the cyclooxygenase activity is measured using a radiometric assay, and the specific activity of the final enzyme preparations used is between 20,000 and 35,000 units. Ketorolac (2 -15 μL) are diluted in DMSO and preincubated with the appropriate recombinant COX (3 -15 ng) at a final concentration of 0.01 to 1000 μM in a reaction mixture (150 μL) containing 50 mM Tris-HCl buffer (pH 7.9), 2 mM EDTA, 10% glycerol, 2 mM phenol, and 1 μM hematin for 10 minutes. The reaction is initiated by addition of [14C]arachidonic acid (50–60 mCi/mmol in a final concentration of 20 μM) and is terminated 45 seconds later by the addition of 100 μL of 0.2 N HCl and 750 μL of distilled water. The total reaction volume is then applied to a 1 mL C18 Sep-pak column that has previously been washed with 2 mL of methanol followed by 5 mL of deionized water. Oxygenated products are eluted with 3 mL of a mixture of acetonitrile/water/acetic acid (50:50:0.1, v/v/v) and quantified by liquid scintillation spectroscopy.
Cell Research:[3]
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  • Cell lines: Primary human osteoblasts cell lines
  • Concentrations: Dissolved in DMSO, final concentration ~0.1 mM
  • Incubation Time: 24 hours
  • Method: Human osteoblasts cells are exposed to Ketorolac for 24 hours. Thymidine incorporation is assessed by the TopCount Microplate Scintillation and Luminescence Counters through adding [3H]-thymidine to cultures 4 hours prior to harvesting. Cell cycle distribution is determined by using propidium iodide in flow cytometer, and cell apoptosis or necrosis is detected using the Annexin V-FITC Apoptosis Detection Kit.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Male Wistar rats
  • Dosages: 0.3-30 mg/kg
  • Administration: Take orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (293.8 mM)
Ethanol 75 mg/mL warmed (293.8 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 255.27


CAS No. 74103-06-3
Storage powder
in solvent
Synonyms N/A
Smiles C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04570878 Recruiting Procedure: SC TAP|Procedure: Control Congenital Heart Disease Seoul National University Hospital January 15 2021 Not Applicable
NCT04227704 Recruiting Drug: Ketamine 50 MG/ML|Drug: Control Postpartum Depression Washington University School of Medicine November 12 2020 Phase 3
NCT04495894 Recruiting Drug: Preoperative Ketorolac Non-small Cell Lung Cancer|Renal Cell Carcinoma Emory University August 24 2020 Early Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID