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GSK5852

Cat. No. M28183
GSK5852 Structure
Synonym:

GSK2485852

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Biological Activity

GSK5852 (GSK2485852) is an HCV NS5B polymerase inhibitor, with an IC50 value of 50 nM. GSK5852 displays antiviral activity and inhibits HCV with EC50s of 3.0 nM (genotype 1a, GT1a) and 1.7 nM (GT1b), respectively.

Chemical Information
Molecular Weight 554.37
Formula C27H25BF2N2O6S
CAS Number 1331942-30-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Peng Zhan, et al. J Med Chem. Resurrecting the Condemned: Identification of N-Benzoxaborole Benzofuran GSK8175 as a Clinical Candidate with Reduced Metabolic Liability

[2] Pek Y Chong, et al. J Med Chem. Design of N-Benzoxaborole Benzofuran GSK8175-Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV Inhibitor

[3] David A Wilfret, et al. Clin Pharmacol Drug Dev. A randomized, double blind, dose escalation, first time in human study to assess the safety, tolerability, pharmacokinetics, and antiviral activity of single doses of GSK2485852 in chronically infected hepatitis C subjects

[4] Christian Voitenleitner, et al. Antimicrob Agents Chemother. In vitro characterization of GSK2485852, a novel hepatitis C virus polymerase inhibitor

[5] Andrew Maynard, et al. J Med Chem. Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase

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Keywords: GSK5852, GSK2485852 supplier, Anti-infection, inhibitors, activators

 
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