Helioxanthin derivative 5-4-2 Chemical Properties

Melting point:

252-254 °C

Boiling point:

671.3±55.0 °C(Predicted)

Density 

1.491±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

pka

13.14±0.20(Predicted)

color 

White to off-white

Helioxanthin derivative 5-4-2 Usage And Synthesis

Uses

Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells. IC50 value: 0.08 uM (EC50) [1][2] Target: Anti-HBV Helioxanthin derivative 5-4-2 had potent anti-HBV activities in HepG2.2.15 cells, with the EC50s of 1 and 0.08 microM, respectively. The lamivudine-resistant HBV, L526M/M550V double mutant strain, was also sensitive to helioxanthin and 5-4-2. This class of compounds not only inhibited HBV DNA, but also decreased HBV mRNA and HBV protein expression. The EC50 of HBV DNA inhibition was consistent with the EC50 of HBV 3.5 Kb transcript inhibition, which was 1 and 0.09 microM for helioxanthin and 5-4-2 respectively.

Biological Activity

helioxanthin derivative 5-4-2, an analogue of helioxanthin (ach126447), is a small-molecule inhibitor of hbv, hsv-1and hsv-2 virus with ec50 values of 0.08 μm, 0.29 μm and 0.16 μm, respectively [1].helioxanthin derivative 5-4-2 is a lactam and has been reported to inhibit the hbv dna and rna and viral protein expression [2]. helioxanthin derivative 5-4-2 has significant anti-virus activity with ec50 values of 0.08 μm, 0.29 μm and 0.16 μm for hbv(hepatitis b virus), hsv-1(herpes simplex virus type 1) and hsv-2(herpes simplex virus type 2), respectively [1]. in addition, helioxanthin derivative 5-4-2 inhibited hbv replication by post-transcriptional down-regulation of necessary transcription factors [3]. helioxanthin derivative 5-4-2 has also exhibited potent anti-hcv (hepatitis c virus) activity with 55% inhibition at 1.0 μm and 80%inhibition at 3.0 μm [1].

References

[1] yeo h1, li y, fu l, zhu jl, gullen ea, dutschman ge, lee y, chung r, huang es, austin dj, cheng yc. synthesis and antiviral activity of helioxanthin analogues. j med chem. 2005 jan 27;48(2):534-46.
[2] li y1, fu l, yeo h, zhu jl, chou ck, kou yh, yeh sf, gullen e, austin d, chengyc.inhibition of hepatitis b virus gene expression and replication by helioxanthin and its derivative. antivir chem chemother. 2005;16(3):193-201.
[3] stein ll1, loomba r. drug targets in hepatitis b virus infection. infect disord drug targets. 2009 apr;9(2):105-16.

Helioxanthin derivative 5-4-2(203935-39-1)Related Product Information

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