Bay 41-4109 (Bayer 41-4109) |
| カタログ番号GC32065 |
BAY 41-4109 は、53 nM の IC50 を持つヒト B 型肝炎ウイルス (HBV) の強力な阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 298708-81-3
Sample solution is provided at 25 µL, 10mM.
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BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
BAY 41-4109 is able to both accelerate and misdirect capsid assembly in vitro. Preformed capsids are stabilized by BAY 41-4109, up to a ratio of one inhibitor molecule per two dimers[2]. BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level, with IC50s of 32.6 and 132 nM in HepG2.2.15 cells, respectively. HBV DNA and HBcAg are inhibited in a dose-dependent manner, indicating that the anti-HBV mechanisms are associated with and dependent on the rate of HBcAg inhibition[3].
BAY 41-4109 reduces viral DNA in the liver and in the plasma dose-dependently with efficacy comparable to 3TC. BAY 41 -4109 reduces hepatitis B virus core antigen (HBcAg) in livers of HBV-transgenic mice. Pharmacokinetic studies in mice have shown rapid absorption, a bioavailability of 30% and dose-proportional plasma concentrations, about 60% in rats and dogs[1].BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid[2].
[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.
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]. |
References: [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. | |
| Cas No. | 298708-81-3 | SDF | |
| Canonical SMILES | O=C(C1=C(C)N=C(C2=NC=C(F)C=C2F)N[C@H]1C3=CC=C(F)C=C3Cl)OC | ||
| Formula | C18H13ClF3N3O2 | M.Wt | 395.76 |
| 溶解度 | DMSO : 100 mg/mL (252.68 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5268 mL | 12.6339 mL | 25.2678 mL |
| 5 mM | 0.5054 mL | 2.5268 mL | 5.0536 mL |
| 10 mM | 0.2527 mL | 1.2634 mL | 2.5268 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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