酮咯酸氨丁三醇
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分子式 C15H13NO3·C4H11NO3 分子量376.40 MDL号 MFCD00887595 PubChem编号 24278503 属性 熔点 160-162 °C 溶解性 Soluble in ethanol (~7 mg/ml)
| 货号 | CAS号 | 操作 |
|---|---|---|
| K129289-5g | 74103-07-4 | 询底价 |
| K129289-1g | 74103-07-4 | 询底价 |
耗材描述
- 分子式 C15H13NO3·C4H11NO3
- 分子量376.40
- MDL号 MFCD00887595
- PubChem编号 24278503
属性
| 熔点 | 160-162 °C |
| 溶解性 | Soluble in ethanol (~7 mg/ml), DMF (~50 mg/ml), DMSO (~7 mg/ml), water (15 mg/ml), and methanol. |
| 存贮条件 | 储存温度 2-8°C |
描述
| 应用 | A non selective inhibitior of Cox-1 and Cox-2. |
| 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. |
| 备注 | Ketorolac (Ketorolac tromethamine, Toradol) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. |
| 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. |
| 别名 | 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;Toradol;(±)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid tris salt; Ketorolac Tromethamine |
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