1. Anti-infection
  2. HBV

Bay 41-4109 (Synonyms: Bayer 41-4109)

Cat. No.: HY-100029 Purity: 98.92% ee.: 99.52%
Handling Instructions

BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.

For research use only. We do not sell to patients.

Bay 41-4109 Chemical Structure

Bay 41-4109 Chemical Structure

CAS No. : 298708-81-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 345 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of Bay 41-4109:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.

IC50 & Target

IC50&Target: 53 nM (HBV)[1]

In Vitro

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].

In Vivo

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].

References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[3]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

395.76

Formula

C₁₈H₁₃ClF₃N₃O₂

CAS No.

298708-81-3

SMILES

O=C(C1=C(C)N=C(C2=NC=C(F)C=C2F)N[[email protected]]1C3=CC=C(F)C=C3Cl)OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Bay 41-4109
Cat. No.:
HY-100029
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