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BMS-986144

Cat. No. M21290
BMS-986144  Structure
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Biological Activity

BMS-986144 is a third generation pan-genotypic NS3/4A protease inhibitor.BMS-986144 inhibits GT-1a, GT-1b, GT-2a, GT-3a, 1a R155X, 1b D168V replicon with EC50 values of 2.3, 0.7, 1.0, 12, 8.0, 5.8 nM, respectively.BMS-986144 has the potential to study HCV infection.

Chemical Information
Molecular Weight 856.94
Formula C40H48D3F4N5O9S
CAS Number 1606150-08-6
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] Li-Qiang Sun, et al. J Med Chem. Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection

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