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GS-9256

Cat. No. M2727
GS-9256 Structure
Size Price Availability
10mg USD 220  USD220 Out of stock
50mg USD 780  USD780 Out of stock
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Quality Control & Documentation
Biological Activity

GS-9256 is a novel phosphinic acid derived inhibitor of the HCV NS3/4A protease with IC50 of 4 nM.

Chemical Information
Molecular Weight 957.46
Formula C46H56ClF2N6O8PS
CAS Number 1001094-46-7
Solubility (25°C) DMSO
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] Hongmei Mo, et al. Antiviral response and resistance analysis of treatment-naïve HCV infected patients receiving multiple doses of the NS3 protease inhibitor GS-9256

[2] Huiling Yang, et al. Preclinical characterization of the novel HCV NS3 protease inhibitor GS-9256

[3] Ona Barauskas, et al. Binding kinetics, potency, and selectivity of the hepatitis C virus NS3 protease inhibitors GS-9256 and vedroprevir

[4] X Christopher Sheng, et al. Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity

[5] Stefan Zeuzem, et al. The protease inhibitor, GS-9256, and non-nucleoside polymerase inhibitor tegobuvir alone, with ribavirin, or pegylated interferon plus ribavirin in hepatitis C

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Keywords: GS-9256 supplier, HCV Protease, inhibitors, activators


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