Name: Ketorolac
Brand: Selleck Chemicals
SKU: S1646
Availability: InStock
Rating: 5 (3 reviews)

Jump to

Quality Control

Batch: Purity: 99.39%

99.39

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other COX Inhibitors	NS-398 (NS398) Paeoniflorin (NSC 178886) Lumiracoxib Xanthohumol Bufexamac Nimesulide Ginsenoside Rd Oroxin B Phenacetin Tolfenamic Acid

Solubility

In vitro
Batch:

DMSO : 51 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 51 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (14.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	255.27	Formula	C₁₅H₁₃N₁O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	74103-06-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O

Mechanism of Action

Features	A COX-1 preferential inhibitor among currently marked nonsteroidal anti-inflammatory drugs (NSAIDs).
Targets/IC₅₀/Ki	COX-1 (human) 1.23 μM COX-2 (human) 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. This compound 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 this chemical 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. It 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. This compound 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.
Kinase Assay	Inhibition of Prostaglandin Formation
Kinase Assay	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.
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. This compound 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%. It does not significantly affect COX-2 activity at doses of ≤3 mg/kg, but at doses of 10 and 30 mg/kg, it produces significant inhibition of COX-2 activity by 75% and 91%, respectively. This chemical causes gastric damage in rats only at doses that inhibits both COX-1 and COX-2, or when given with a COX-2 inhibitor.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10027870/ [2] https://pubmed.ncbi.nlm.nih.gov/10450786/ [3] https://pubmed.ncbi.nlm.nih.gov/19428934/ [4] https://pubmed.ncbi.nlm.nih.gov/10982765/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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

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

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):

Ketorolac COX inhibitor

Chemical Structure

Molecular Weight: 255.27