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GS-9451

Cat. No. M3680

GS-9451 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GS-9451 is a potent macrocyclic HCV NS3 PI that achieved a median maximal change in HCV RNA of 3.6 log10 IU/mL (range, -4.7 log10 to -3.1 log10 IU/mL) following 3-day monotherapy in treatment-naïve patients with HCV genotype 1 infection during phase I. In multiple GT1a and GT1b replicon cell lines, GS-9451 had mean 50% effective concentrations (EC50s) of 13 and 5.4 nM, respectively, with minimal cytotoxicity; similar potency was observed in chimeric replicons encoding the NS3 protease gene of GT1 clinical isolates. GS-9451 was less active in GT2a replicon cells (EC50 = 316 nM). GS-9451 showed good oral bioavailability in all three species tested.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight
Formula
CAS Number 1310824-24-8
Purity >99%
Solubility
Storage at -20°C
References

Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451.
Yang H, et al. Antimicrob Agents Chemother. 2014;58(2):647-53. PMID: 23939899.

Characterization of resistance to the protease inhibitor GS-9451 in hepatitis C virus-infected patients.
Dvory-Sobol H, et al. Antimicrob Agents Chemother. 2012 Oct;56(10):5289-95. PMID: 22869562.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GS-9451 supplier, HCV Protease, inhibitors

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