Bay 41-4109 racemate

An antiviral agent

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库存: 现货

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数量
1mg

￥312.00

250.00

- +
5mg

￥762.00

610.00

- +
10mg

￥1300.00

1040.00

- +
50mg

￥4100.00

3280.00

- +
100mg

￥6475.00

5180.00

- +

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金额: ￥0.00

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Background

(±)-BAY 41-4109 is a heteroaryldihydropyrimidine with antiviral activity.¹ It inhibits hepatitis B virus (HBV) replication in HepG2.2.15 cells (IC₅₀ = 202 nM) without affecting cell growth. (±)-BAY 41-4109 (25 mg/kg) reduces viral replication and viral load in a humanized mouse model of HBV infection.

1.Brezillon, N., Brunelle, M.-N., Massinet, H., et al.Antiviral activity of Bay 41-4109 on hepatitis B virus in humanized Alb-uPA/SCID micePLoS One6(12)e25096(2011)

Protocol

Cell experiment:

Cellular metabolism is evaluated by MTT colorimetry. HepG2.2.15 cells are plated at a density of 2 × 103 cells per well in 96-well plates. After 8 d of treatment with different concentrations of each antiviral compound, 20 μL of MTT solution (5 g/L) are added to each well and incubated at 37°C for 4 h. Next, 150 μL of DMSO is added and stirred for 10 min to dissolve the crystals. Absorbance values are recorded at 490 nm by using an ELISA reader. The MTT values are calculated using the curve regression equation[3].

Animal experiment:

Mice: The HBV-transgenic mice are used in the study. Compounds (BAY 41-4109) are formulated as a suspension in 0.5% Tylose and administered per os to mice two times/day for a 28 day period. The 0.5% Tylose serves as a placebo. Six hours after the last treatment, the animals are sacrificed and livers are removed and immediately frozen for subsequent analysis. Blood is obtained by cardiac puncture of the anesthesized animals[1].

参考文献:

[1]. Weber O, et al. Inhibition of human hepatitis B virus (HBV) by a novel non-nucleosidic compound in a transgenic mouse model. Antiviral Res. 2002 May;54(2):69-78.
[2]. Stray SJ, et al. BAY 41-4109 has multiple effects on Hepatitis B virus capsid assembly. J Mol Recognit. 2006 Nov-Dec;19(6):542-8.
[3]. Wu GY, et al. Inhibition of hepatitis B virus replication by Bay 41-4109 and its association with nucleocapsid disassembly. J Chemother. 2008 Aug;20(4):458-67.