| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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Purity: ≥98%
Ketorolac (Toradol, Acular, RS 37619; RS37619; Sprix, Macril, Acuvail, Lixidol), an NSAID (non-steroidal anti-inflammatory drug), is a potent and non-selective COX inhibitor of COX-1 and COX-2 with potential anti-inflammatory activity. It inhibits COX-1/2 with IC50s of 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. 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.
| ln Vitro |
The oral cancer cells can be successfully killed by ketorolac (RS37619) salt (0-30 μM; 48 h)[4]. In H357 cells, ketorolac salt (0–5 μM; 48 h) causes apoptosis and suppresses the production of the DDX3 protein[4]. Oral cancer cell growth is inhibited by ketorolac salt (0-2.5 μM; 0-16 h)[4]. By directly interacting with DDX3, ketorolac salt (0–50 μM) suppresses ATPase activity[4].
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| ln Vivo |
In rabbits, ketorolac (RS37619), or 0.4% ketorolac tromethamine ophthalmic solution, exhibits potent anti-inflammatory effects on the eyes[1]. Rats' alveolar socket volume fraction of bone trabeculae is unaffected negatively by ketorolac (4 mg/kg/day, po; 2 weeks)[2]. In rats, intrathecal injection of ketorolac (60 μg) attenuates the damage induced by spinal cord ischemia[3]. Mice exposed to ketorolac salt (20 and 30 mg/kg; ip; twice weekly for three weeks) have less oral carcinogenesis[4].
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| Cell Assay |
Cell Viability Assay [4]
Cell Types: HOK, SCC4, SCC9 and H357 cells Tested Concentrations: 0-30 μM Incubation Duration: 48 h Experimental Results: demonstrated inhibition with IC50s of 2.6, 7.1 and 8.1 μM against H357, SCC4 and SCC9 cells, respectively. And the normal HOK cell line did not show any cell death effect. Cell Proliferation Assay[4] Cell Types: H357 Tested Concentrations: 0.5, 1.0, 1.5, 2.0 and 2.5 μM Incubation Duration: 0, 8 and 16 h Experimental Results: Inhibited the proliferation. Western Blot Analysis[4] Cell Types: H357 Tested Concentrations: 1, 2.5 and 5 μM Incubation Duration: 48 h Experimental Results: Dramatically decreased DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin. Apoptosis Analysis[4] Cell Types: H357 Tested Concentrations: 2.5 and 5 μM Incubation Duration: 48 h Experimental Results: Induced apoptosis. |
| Animal Protocol |
Animal/Disease Models: New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation[1]
Doses: 50 μL ketorolac tromethamine ophthalmic solution 0.4% Route of Administration: In eyes, twice, 2 hrs (hours) and 1 hour before LPS challenge Experimental Results: Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE2 concentrations in the aqueous humor. Animal/Disease Models: Male Wistar rats (400–450 g), spinal cord ischemia model[3] Doses: 30 and 60 μg Route of Administration: Intrathecal injection , 1 h before the ischemia induction for once Experimental Results: Dramatically decreased the motor disturbances and improved the survival rate at 60 μg. Animal/Disease Models: Dramatically decreased the motor disturbances and improved the survival rate at 60 μg. Doses: 20 mg/kg and 30 mg/kg Route of Administration: IP injection, two times in a week for 3 weeks |
| References |
[1]. Waterbury LD, et al. Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40.
[2]. Fracon RN, et al. Treatment with paracetamol, ketorolac or etoricoxib did not hinder alveolar bone healing: a histometric study in rats. J Appl Oral Sci. 2010 Dec;18(6):630-4. [3]. Hsieh YC, et al. Intrathecal ketorolac pretreatment reduced spinal cord ischemic injury in rats. Anesth Analg. 2005 Apr;100(4):1134-9. [4]. Samal SK, et al. Ketorolac salt is a newly discovered DDX3 inhibitor to treat oral cancer. Sci Rep. 2015 Apr 28;5:9982. |
| Molecular Formula |
C15H13N1O3
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| Molecular Weight |
255.27
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| CAS # |
74103-06-3
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| Related CAS # |
Ketorolac tromethamine salt;74103-07-4;(S)-Ketorolac;66635-92-5;(R)-Ketorolac;66635-93-6;Ketorolac-d5;1215767-66-0;Ketorolac hemicalcium;167105-81-9;Ketorolac-d4;1216451-53-4
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| SMILES |
O([H])C(C1([H])C2=C([H])C([H])=C(C(C3C([H])=C([H])C([H])=C([H])C=3[H])=O)N2C([H])([H])C1([H])[H])=O
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| InChi Key |
OZWKMVRBQXNZKK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13/h1-7,11H,8-9H2,(H,18,19)
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| Chemical Name |
5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9174 mL | 19.5871 mL | 39.1742 mL | |
| 5 mM | 0.7835 mL | 3.9174 mL | 7.8348 mL | |
| 10 mM | 0.3917 mL | 1.9587 mL | 3.9174 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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