1. Metabolic Enzyme/Protease
  2. Lipoxygenase
  3. CMI-392

CMI-392是一种双重 5-lipoxygenese 抑制剂和血小板活化因子 (PAF) 受体拮抗剂,IC50 值分别为100和10 nM。

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CMI-392 Chemical Structure

CMI-392 Chemical Structure

CAS No. : 205654-37-1

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查看 Lipoxygenase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.

IC50 & Target

5-LO

100 nM (IC50)

PAF

10 nM (IC50)

体内研究
(In Vivo)

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 1.8 mg/kg, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

633.15

Formula

C31H37ClN2O8S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Kinase Assay
[1]

5-lipoxygenese activity in cell lysate is determined as follows: 0.1 mL 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 (20 min, room temperature). A substrate mix containing [14C]AA is added and incubated further (5 min, 37°C). The reaction is terminated by adding 0.2 mL of an organic extraction solution containing triphenylphosphine, followed by microcentrifugation. The organic phase (50 μL) 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 36 h. The film is developed and scanned using a densitometer, and the peak areas of AA and its products are calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Acute TPA-induced ear edema in mice is determined by topically applying TPA to the ears of mice. Mice are sacrificed after 6 h 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CMI-392
目录号:
HY-19205A
需求量: