Home Neuronal Signaling COX inhibitor Ketorolac For research use only.

Ketorolac

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

Ketorolac Chemical Structure

Ketorolac Chemical Structure

CAS No. 74103-06-3

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Ketorolac Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

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).
Targets
COX-1 (human) [1] COX-2 (human) [1]
1.23 μM 3.50 μM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Male Wistar rats
Dosages 0.3-30 mg/kg
Administration Take orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05776953 Recruiting
Renal Colic|Flank Pain|Emergencies|Analgesia
Hackensack Meridian Health
 December 21 2023 Phase 4
NCT05336968 Recruiting
Osteoarthritis Knee
United Health Services Hospitals Inc.
 September 15 2022 Phase 4
NCT05336266 Recruiting
Pancreas Cancer|Pancreatic Ductal Adenocarcinoma|Pancreatic Cancer
Andrew Hendifar MD|Yinuoke Ltd.|Cedars-Sinai Medical Center
 July 1 2022 Early Phase 1

Chemical Information & Solubility

Molecular Weight 255.27 Formula

C15H13N1O3
CAS No. 74103-06-3 SDF Download Ketorolac SDF
Smiles C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (293.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 75 mg/mL

Ethanol : 75 mg/mL


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In vivo
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