中文名称 |
酮咯酸氨丁三醇; (+/-)-5-苯甲酰基-2,3-二氢-1H-吡咯里嗪-1-甲酸氨丁三醇盐 |
英文名称 |
Toradol;(±)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid tris salt; Ketorolac Tromethamine |
CAS识别号 |
74103-07-4 |
MDL识别号 |
MFCD00887595 |
EC识别号 |
Null,without related properties. |
Beilstein |
Null,without related properties. |
分子式 |
C15H13NO3·C4H11NO3 |
分子量 |
376.40 |
分子结构图 |
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产品性状 |
溶解性:Soluble in ethanol (~7 mg/ml), DMF (~50 mg/ml), DMSO (~7 mg/ml), water (15 mg/ml), and methanol. |
质量标准 |
产品介绍 |
Ketorolac (tromethamine salt) inhibits both isoforms of Cox in recombinant rat and human enzyme systems. Ketorolac inhibits rat Cox-1 (IC50 of 0.27 μM), rat Cox-2 (IC50 of 2.06 μM), human Cox-1 (IC50 of 1.23 μM) and human Cox-2 (IC50 of 3.50 μM). The (S) enantiomer of Ketorolac with rat Cox-1 (IC50 of 0.10 μM) is approximately twice as potent as the racemate, whereas the (R)-enantiomer (IC50 of 100 μM) is virtually without activity. Ketorolac shows inhibition of eicosanoid formation in HEL cells (Cox-1, IC50 of 0.025 μM) and LPS-stimulated Mono Mac 6 cells (Cox-2, IC50 of 0.039 μM), but does not significantly inhibit NO accumulation in supernatants of LPS-stimulated RAW 264.7 cells up to 300 μM. 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. |
用途 |
A non selective inhibitior of Cox-1 and Cox-2. |
生化机理 |
Non-steroidal anti-inflammatory agent and cyclooxygenase (COX) inhibitor that is relatively selective for COX-1. Inhibits the induction of nitric oxide synthase by lipopolysaccharide in a murine macrophage cell line. Part of its analgesic effect may be due to the release of opioid peptides. |
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储存条件 |
2-8 °C 冷藏保存,Stored at 2-8 °C. |