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PGS-IN-1(KME-4)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PGS-IN-1(KME-4)图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
PGS-IN-1 (KME-4) 是一种有效的前列腺素合成酶 (PGS) 抑制剂,IC50 为 0.28 μM;也抑制 5-脂氧合酶,IC50 为 1.05 μM.

Kinase experiment:

PGS-IN-1 is dissolved in ethanol and the final concentration of ethanol is kept at 2% in each assay. The reaction mixture includes reaction buffer, enzyme (20 μg protein), and PGS-IN-1 in a total volume of 0.2 mL. The mixture is incubated for 15 min at 37℃ with shaking and terminated by the addition of 2.5 mL ethyl acetate and 25 μL 1 N formic acid[1].

Animal experiment:

Rats: PGS-IN-1 is administered orally to groups of 4-6 male Wistar rats weighting 160-220 g. One hour later, 1 % carrageenin in 0.9 % NaCl is injected subcutaneously into a hind paw. Paw volumes are measured 5 h after the injection[1].

产品描述

PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.

The synthesized α-benzulidene-γ-butyrolactones are pure isomers (either cis or trans). PGS-IN-1 is the trans isomer. PGS-IN-1 exhibits potent antiinflammatrory and PGS inhibitory activity (IC50=0.28 μM). PGS-IN-1 also shows potent inhibitory activity against 5-lipoxygenase (IC50=1.05 μM)[1].

[1]. Katsumi I, et al. Studies on styrene derivatives. I. Synthesis and antiinflammatory activities of alpha-benzylidene-gamma-butyrolactone derivatives. Chem Pharm Bull (Tokyo). 1986 Jan;34(1):121-9.