Name | α-(3,5-di-tert-butyl-4-hydroxybenzylidene)-γ-butyrolactone |
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Synonyms | PGS-IN-1 |
Description | 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. |
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Related Catalog | |
Target |
IC50: 0.28 μM (PGS), 1.05 μM (5-lipoxygenase)[1] |
In Vitro | 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]. |
Kinase Assay | 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°C with shaking and terminated by the addition of 2.5 mL ethyl acetate and 25 μL 1 N formic acid[1]. |
Animal Admin | 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]. |
References |
Molecular Formula | C19H26O3 |
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Molecular Weight | 302.40800 |
Exact Mass | 302.18800 |
PSA | 46.53000 |
LogP | 4.31750 |
Hazard Codes | Xi |
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Precursor 0 | |
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DownStream 1 | |