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Formula | C15H13N1O3 |
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Molecular Weight | 255.27 | CAS No. | 74103-06-3 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 75 mg/mL (293.8 mM) | ||||||||
Ethanol | 75 mg/mL (293.8 mM) | ||||||||||
Water | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. | ||||
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Targets |
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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. (R, S)-Ketorolac 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 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. [1] 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, but does not significantly inhibit NO accumulation in supernatants of LPS-stimulated RAW 264.7 cells up to 300 μM. [2] Ketorolac 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. [3] | ||||
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. [1] Ketorolac 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%. Ketorolac does not significantly affect COX-2 activity at doses of ≤3 mg/kg, but at doses of 10 and 30 mg/kg, Ketorolac produces significant inhibition of COX-2 activity by 75% and 91%, respectively. Ketorolac causes gastric damage in rats only at doses that inhibits both COX-1 and COX-2, or when given with a COX-2 inhibitor. [4] | ||||
Features | A COX-1 preferential inhibitor among currently marked nonsteroidal anti-inflammatory drugs (NSAIDs). |
Kinase Assay:[1] |
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Cell Assay:[3] |
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Animal Study:[4] |
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Postoperative Administration of Ketorolac Averts Morphine-Induced Angiogenesis and Metastasis in Triple-Negative Breast Cancer [ Life Sci, 2020, 15;251:117604] | PubMed: 32243929 |
Ribosomal Protein L13 Promotes IRES-Driven Translation of Foot-and-Mouth Disease Virus in a Helicase DDX3-Dependent Manner [ J Virol, 2020, 6;94(2):e01679-19] | PubMed: 31619563 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.