Ketorolac

Catalog No.S1646

Ketorolac Chemical Structure

Molecular Weight(MW): 255.27

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

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 197 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective COX Inhibitors

Biological Activity

Description Ketorolac (Ketorolac tromethamine) 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

(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]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Male Wistar rats
  • Formulation: Dissolved in DMSO and diluted in saline.
  • 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
Formula

C15H13N1O3

CAS No. 74103-07-4
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03007381 Not yet recruiting Breast Cancer Female Nova Scotia Health Authority July 2017 Phase 4
NCT02973958 Not yet recruiting Pain, Postoperative|Phimosis|Paraphimosis|Balanitis Alberta Childrens Hospital February 2017 Phase 1
NCT03032458 Recruiting Analgesia|Urolithiasis Mansoura University January 2017 Phase 4
NCT03025594 Recruiting Knee Arthroplasty|Pain Management maximiliano barahona vasquez|University of Chile January 2017 Phase 3
NCT02987920 Not yet recruiting Pain, Postoperative University of Southern California January 2017 Phase 4
NCT02940405 Not yet recruiting Irreversible Pulpitis Cairo University January 2017 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

COX Signaling Pathway Map

Related COX Products

Tags: buy Ketorolac | Ketorolac supplier | purchase Ketorolac | Ketorolac cost | Ketorolac manufacturer | order Ketorolac | Ketorolac distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID