中文名称: CMI-392
英文名称: CMI-392
CAS No: 205654-37-1
分子式: C31H37ClN2O8S
分子量: 633.15
C11239 CMI-392 (psaitong)
包装规格:
100mg in glass bottle
产品描述:

基本信息

产品编号:

C11239

产品名称:

CMI-392

CAS:

205654-37-1

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C31H37ClN2O8S

溶于液体

 

 

分子量

633.15

 

 

化学名: 

 

 

生物活性

产品描述

一种双重5-lipoxygenese抑制剂和血小板活化因子(PAF)受体拮抗剂。

靶点

5-LO

100nM (IC50)

PAF

10nM (IC50)

体内研究

Topical treatment of CMI-392 in the acute and chronic TPA models result in a significant decrease of ear weight, inflammatory cell infiltration, and histological examination. The ED50 for PAF-induced mouse hemoconcentration and arachidonic acid-induced mouse ear edema are 2.2 and 1.8mg/kg, respectively

 

推荐实验方法(仅供参考)

Kinase Assay

5-lipoxygenese activity in cell lysate is determined as follows: 0.1mL reactions consisting of buffer, test compound (CMI-392 in DMSO), and an amount of cell lysate that will convert 15% of [14C]AA substrate mix to oxygenated products are incubated (20min, room temperature). A substrate mix containing [14C]AA is added and incubated further (5min, 37°C). The reaction is terminated by adding 0.2mL of an organic extraction solution containing triphenylphosphine, followed by microcentrifugation. The organic phase (50μL) is spotted onto silica gel TLC plates. The plates are developed in ethyl ether/acetic acid (100:0.1) (25 min, room temperature). Plates are exposed to film for 36h. The film is developed and scanned using a densitometer, and the peak areas of AA and its products are calculated

 

 

Animal Administration

Mice: Acute TPA-induced ear edema in mice is determined by topically applying TPA to the ears of mice. Mice are sacrificed after 6h and the ear punch biopsies are weighed. Chronic TPA-induced ear edema in mice is determined by topically applying TPA once a day every 2 days for a total of 10 days. CMI-392 is topically administered twice daily on the last 3 days of the experiment. Mice are then sacrificed and the ear punch biopsies are weighed. Biopsies are homogenized and MPO content is determined via spectrophotometric assay

保存条件:
-20℃
UN码:
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