酮咯酸氨丁三醇

中文名称:

酮咯酸氨丁三醇

中文同义词:

(+/-)-5-苯甲酰基-2,3-二氢-1H-吡咯里嗪-1-甲酸氨丁三醇盐;辛太克斯(浮选剂);酮咯酸氨丁三醇;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;安贺拉PF;酮咯酸三醇;酮咯酸氨三丁醇;酮咯酸氨丁三醇(标准品)

英文名称:

Ketorolac tromethamine

英文同义词:

KETOROLAC TRIS SALT;KETOROLAC TROMETHAMINE;KETOROLAC TROMETHAMINE SALT;(+/-)-5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID, TRIS (HYDROXYMETHYL) AMINOMETHANE SALT;(+/-)-5-benzoyl-2,3-dihydro-1h-pyrrolizine-1-carboxylic acid tris(hydroxymethyl)methylamine salt;(+/-)-5-BENZOYL-2,3-DIHYDRO-1H-PYRROLIZINE-1-CARBOXYLIC ACID TRIS SALT;KETROLAC TROMETHAMINE SALT;(±)-Form tromethamine salt

CAS号:

74103-07-4

分子式:

C19H24N2O6

分子量:

376.4

EINECS号:

相关类别:

神经信号;医药中间体;小分子抑制剂;水电平衡及透析用药物;医药与生物化工;原料药;医药原料;Aromatics;Heterocycles;Other APIs;化合物：原料药;11;医药产品;中间体;眼科类药物;醇类;医药原料药;医药、农药及染料中间体;化工原料;杂质对照品;化学试剂;Inhibitors;Intermediates Fine Chemicals;Pharmaceuticals;Pharmaceutical raw material;API;Acular

Mol文件:

74103-07-4.mol

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

最大波长(λmax)

322nm(MeOH)(lit.)

Merck 

14,5306

InChIKey

BWHLPLXXIDYSNW-UHFFFAOYSA-N

CAS 数据库

74103-07-4(CAS DataBase Reference)

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

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.

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

HazardClass 

6.1(a)

PackingGroup 

II

海关编码 

2933995500