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HBF-0259

Cat. No. M10829
HBF-0259  Structure
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Biological Activity

HBF-0259 is a potent and selective hepatitis B virus (HBV) surface antigen (HBsAg) secretion inhibitor in HepG2.2.15 cells EC50 The value is 1.5 μM. HBF-0259 has no effect on HBV DNA synthesis.

Chemical Information
Molecular Weight 364.2
Formula C16H12Cl2FN5
CAS Number 957011-15-3
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alireza Mohebbi, et al. Virusdisease. Prediction of HBF-0259 interactions with hepatitis B Virus receptors and surface antigen secretory factors

[2] Wenquan Yu, et al. J Med Chem. Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion

[3] Anne Marie Dougherty, et al. Antimicrob Agents Chemother. A substituted tetrahydro-tetrazolo-pyrimidine is a specific and novel inhibitor of hepatitis B virus surface antigen secretion

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