Ketorolac

SKU: orb1217685

Description

Ketorolac is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 74103-06-3
• MW: 255.27
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₃NO₃
• SMILES: O=C(C1C2=CC=C(C(C3=CC=CC=C3)=O)N2CC1)O
• Target: COX
• Solubility: DMSO: 70 mg/mL (274.22 mM; Need ultrasonic);H2O: 70 mg/mL (274.22 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits. Ketorolac (4 mg/kg/day, p.o. ; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats. Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats. Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice. Animal model: New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation. Dosage: 50 μL ketorolac tromethamine ophthalmic solution 0.4%. Administration: In eyes, twice, 2 hours and 1 hour before LPS challenge. Result: 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 model: Male Wistar rats (400–450 g), spinal cord ischemia model. Dosage: 30 and 60 μg. Administration: Intrathecal injection, 1 h before the ischemia induction for once. Result: Significantly reduced the motor disturbances and improved the survival rate at 60 μg. Animal model: Significantly reduced the motor disturbances and improved the survival rate at 60 μg. Dosage: 20 mg/kg and 30 mg/kg. Administration: IP injection, two times in a week for 3 weeks. Result: Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).
  Read more...
• In Vitro:
  Ketorolac (RS37619) salt (0-30 μM; 48 h) effectively kills the oral cancer cells. Ketorolac salt (0-5 μM; 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells. Ketorolac salt (0-2.5 μM; 0-16 h) inhibits the proliferation of oral cancer cells. Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity. Cell Viability Assay Cell line: HOK, SCC4, SCC9 and H357 cells. Concentration: 0-30 μM. Incubation time: 48 h. Result: Showed 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 Cell line: H357. Concentration: 0.5, 1.0, 1.5, 2.0 and 2.5 μM Incubation time: 0, 8 and 16 h. Result: Inhibited the proliferation. Western blot analysis. Cell line: H357. Concentration: 1, 2.5 and 5 μM Incubation time: 48 h. Result: Significantly reduced DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin. Apoptosis Analysis Cell line: H357. Concentration: 2.5 and 5 μM Incubation time: 48 h. Result: Induced apoptosis.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

?RS37619 | Toradol | Acular | Sprix | Macril | Acuvail

Quick Database Links

Gene Symbol

COX