| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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Purity: ≥98%
Ketorolac tromethamine (RS37619 tromethamine), potent NSAID (non-steroidal anti-inflammatory drug), is a potent and non-selective COX inhibitor of COX-1 and COX-2 with IC50 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 medication ketorolac is a non-steroidal anti-inflammatory. The IC50 values for COX-1 and COX-2, respectively, indicate that the compound is a non-selective COX inhibitor [1].
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| ln Vivo |
The LPS endotoxin-induced rise in anterior chamber FITC-dextran and the rise in PGE2 content in the aqueous humor are nearly entirely inhibited by ketorolac tromethamine (0.4%) [1]. Intravenous ketorolac (30 mg/kg) reverses rats' hyperalgesia quickly. Additionally, ketorolac can lower PGE2 levels in rats and lessen paw PG synthesis and carrageenan-induced hyperalgesia [1]. Rat alveolar socket volume fraction of trabecular bone produced is unaffected by ketorolac (4 mg/kg/day) taken orally [2]. Rat ischemia cell death, including cytoplasmic eosinophilia, cellular disarray, and nuclear pyknosis, is lessened by ketorolac (60 μg/10 μL). Additionally, ketorolac can enhance hind limb motor function, substantially decrease neuronal death, and have a long-term survival rate comparable to the control group [3].
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| 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 |
| Molecular Formula |
C26H28FN3O9
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|---|---|
| Molecular Weight |
545.52
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| CAS # |
74103-07-4
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| Related CAS # |
Ketorolac;74103-06-3;(S)-Ketorolac;66635-92-5;(R)-Ketorolac;66635-93-6
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| SMILES |
InChI=1S/C15H13NO3.C4H11NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)135-4(1-6,2-7)3-8/h1-7,11H,8-9H2,(H,18,19)6-8H,1-3,5H2
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| InChi Key |
2-amino-2-(hydroxymethyl)propane-1,3-diol 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylate
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| InChi Code |
BWHLPLXXIDYSNW-UHFFFAOYSA-N
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| Synonyms |
Acular Godek Sprix Syntex Toradol Ketorolac tromethamine
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
H2O : ~100 mg/mL (~265.67 mM)
DMSO : ≥ 30 mg/mL (~79.70 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (265.67 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8331 mL | 9.1656 mL | 18.3311 mL | |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL | |
| 10 mM | 0.1833 mL | 0.9166 mL | 1.8331 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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