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Ketorolac tromethamine salt

Catalog No.
B1447
Non-selective COX inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
1g
$50.00
In stock
5g
$230.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Ketorolac (Ketorolac tromethamine, Toradol) is a non-selective COX inhibitor with strong analgesic activity.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt376.4
Cas No.74103-07-4
FormulaC19H24N2O6
Solubility≥13.1 mg/mL in DMSO; ≥9.9 mg/mL in EtOH with ultrasonic; ≥92.8 mg/mL in H2O
Chemical Name2-amino-2-(hydroxymethyl)propane-1,3-diol;5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
SDFDownload SDF
Canonical SMILESC1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

HEL, Mono Mac 6 and RAW 264.7 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.025 ~ 300 μM

Applications

In HEL cells (COX-1) and LPS-induced Mono Mac 6 cells (COX-2), Ketorolac tromethamine salt inhibited eicosanoid formation with the IC50 value of 0.025 μM and 0.039 μM, respectively. However, in supernatants of LPS-induced RAW 264.7 cells, it did not significantly inhibit NO accumulation at the dose up to 300 μM.
Animal experiment [2]:

Animal models

Male Wistar rats

Dosage form

0.3 ~ 30 mg/kg; p.o.

Applications

At all doses, Ketorolac tromethamine salt significantly inhibited COX-1 activity and gastric PG synthesis. At the doses ≥ 1 mg/kg, Ketorolac tromethamine salt inhibited COX-1 activity by 95% and gastric PG synthesis by > 88%, without causing obvious gastric damage. At the dose ≤ 3 mg/kg, Ketorolac tromethamine salt did not significantly affect COX-2 activity, but at the doses of 10 and 30 mg/kg, it inhibited COX-2 activity by 75% and 91%, respectively. Meanwhile, it caused significant gastric damage as well.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Berg J, Fellier H, Christoph T, Grarup J, Stimmeder D. The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro. Inflamm Res. 1999 Jul;48(7):369-79.

[2]. Wallace JL, McKnight W, Reuter BK, Vergnolle N. NSAID-induced gastric damage in rats: requirement for inhibition of both cyclooxygenase 1 and 2. Gastroenterology. 2000 Sep;119(3):706-14.

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