102271-49-8

102271-49-8 structure
102271-49-8 structure
  • Name: PGS-IN-1
  • Chemical Name: α-(3,5-di-tert-butyl-4-hydroxybenzylidene)-γ-butyrolactone
  • CAS Number: 102271-49-8
  • Molecular Formula: C19H26O3
  • Molecular Weight: 302.40800
  • Catalog: Signaling Pathways Immunology/Inflammation PGE synthase
  • Create Date: 2017-03-20 08:05:36
  • Modify Date: 2025-08-25 15:31:01
  • 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.

Name α-(3,5-di-tert-butyl-4-hydroxybenzylidene)-γ-butyrolactone
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.
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

[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.

Molecular Formula C19H26O3
Molecular Weight 302.40800
Exact Mass 302.18800
PSA 46.53000
LogP 4.31750
Hazard Codes Xi
Precursor  0

DownStream  1

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