酮咯酸氨丁三醇

概述用途生物活性靶点体外研究体内研究酮咯酸氨丁三醇试剂级价格

酮咯酸氨丁三醇

CAS号:74103-07-4
英文名:Ketorolac tromethamine
中文名:酮咯酸氨丁三醇
CBNumber:CB2427540
分子式:C19H24N2O6
分子量:376.41
MOL File:74103-07-4.mol

酮咯酸氨丁三醇化学性质

熔点 :160-161 C
储存条件 :2-8°C
溶解度 :H₂O: 15 mg/mL stable at least one month at −20 °C., soluble
形态 :crystalline
颜色 :White to Light yellow
最大波长(λmax) :322nm(MeOH)(lit.)
Merck :14,5306
稳定性 :Hygroscopic
InChI :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)13;5-4(1-6,2-7)3-8/h1-7,11H,8-9H2,(H,18,19);6-8H,1-3,5H2
InChIKey :BWHLPLXXIDYSNW-UHFFFAOYSA-N
SMILES :C(N)(CO)(CO)CO.C(C1C=CC=CC=1)(C1=CC=C2C(C(=O)O)CCN12)=O
CAS 数据库 :74103-07-4(CAS DataBase Reference)

安全信息

危险品标志 :T
危险类别码 :25-36/37/38-23/24/25
安全说明 :26-45-36/37/39
危险品运输编号 :UN 2811 6.1/PG 3
WGK Germany :3
RTECS号 :UY7759900
危险等级 :6.1(a)
包装类别 :II
海关编码 :2933995500

酮咯酸氨丁三醇性质、用途与生产工艺

概述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.