酮咯酸氨丁三醇
Ketorolac tris salt
| 货号 | 包装规格 | 纯度/级别 | 交货周期 | 价格 | 数量 |
|---|---|---|---|---|---|
| YB27486-1g | 1g | 98% | 现货 | ||
| YB27486-5g | 5g | 98% | 现货 | ||
| YB27486-25g | 25g | 98% | 现货 | ||
| YB27486-100g | 100g | 98% | 现货 |
| 中文名称 | 酮咯酸氨丁三醇 |
|---|---|
| 英文名称 | Ketorolac tris salt |
| 别名 | 托拉多尔, （±）-5-苄基-2,3-二氢-1H-吡咯嗪-1羧酸 三羟甲基氨基甲烷盐 |
| Cas No. | 74103-07-4 |
| MDL No. | MFCD00887595 |
| 精确分子量 | 376.16344 |
| Smiles | C1C(C(O)=O)C2=CC=C(C(C3C=CC=CC=3)=O)N2C1.C(O)C(N)(CO)CO |
| 信号词 | Danger |
|---|---|
| 危险类别(旧) | R25;R36/37/38 |
| 熔点 | 493.2ºC at 760 mmHg |
| 化学稳定性 | 吸湿性 |
| 沸点 | 160-161ºC |
| 海关编码 | 2942000000 |
| 特性 | * |
| 安全说明(旧) | S26-S45 |
| 水溶解性 | H2O: soluble 15 mg/mL, clear, colorless to faintly yellow (stable at least one month at −20 °C.) |
| 符号 | GHS06 |
| 存储要求 | room temp |
| 闪点 | Not applicable |
酮咯酸氨丁三醇是醇类有机物，其生物活性与左旋S（-）有关，可抑制前列腺素生物合成。
用途
咯酸氨丁三醇为吡咯烷羧酸衍生物，是由左旋（-）和右旋（+）异构体组成的消旋体，其右旋S（+）异构体具有止痛作用。
生物活性
Ketorolac tromethamine是一种合成的吡呤环羧酸衍生物，具有消炎、止痛和退热活性。它是非选择性的COX抑制剂，对COX-1和COX-2的IC50值都是20 nM。
靶点
| Target | Value |
|
COX1
() | 20 nM |
|
COX2
() | 20 nM |
体外研究
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC 50 s of 20 nM for COX-1 and 120 nM for COX-2.
体内研究
Ketorolac tromethamine (0.4%) causes nearly complete inhibition on LPS endotoxin-induced increases in FITC-dextran in the anterior chamber, and increases in aqueous PGE2 concentrations in the aqueous humor in rabbits. Ketorolac (30 mg/kg, i.v.) rapidly reverses hyperalgesia in rats. Ketorolac also reduces carrageenan-induced hyperalgesia and paw PG production, and causes reduction in PGE2 levels in rats. Ketorolac (4 mg/kg/day, p.o.) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats. Ketorolac (60 μg/10 μL) reduces the histological changes such as ischemic cell death, including cytoplasmic eosinophilia with disintegration of cytoarchitecture and nuclear pyknosis in rats. Ketorolac also effectively reduces neuronal death and improves hindlimb motor function, and the long-term survival is similar to that in the control group.
