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Amphihevir

Chemical Structure : Amphihevir

CAS No.: 1890171-61-5

Amphihevir

Catalog No.: PC-73081Not For Human Use, Lab Use Only.

Amphihevir is a potent, selective HCV NS4B inhibitor with EC50 of 0.34 and 1.97 nM against the GT1a (H77) and GT1b replicon in luciferase assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Amphihevir is a potent, selective HCV NS4B inhibitor with EC50 of 0.34 and 1.97 nM against the GT1a (H77) and GT1b replicon in luciferase assays.
Amphihevir shows weaker acitivity against GT2a (JFH-1) (EC50=186 nM).
Amphihevir shows EC50 3.13 nM and 18.16 nM with 100% human serum against GT1a and GT1b replicons using HCV-1b replicon cells test.
Amphihevir reduced replicon RNA by nearly 6,300-fold (3.8 log10) at a concentration 25-fold greater than the EC90 (300 nM).
Amphihevir was found to be inactive against other viruses, human kinases, and GPCRs, which implies its good selectivity.
Amphihevir has good oral bioavailability and appropriate T1/2 in rats and dogs, showed good safety profiles in rats and dogs.
Amphihevir is the first reported NS4B inhibitor that has advanced to clinical trials.

Physicochemical Properties

M.Wt 448.402
Formula C21H19F3N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-cyclopropyl-2-(4-(2-oxooxazolidin-3-yl)piperazine-1-carbonyl)-7-(trifluoromethyl)benzofuran-3-carbonitrile

References

1. Xin Tao, et al. Antimicrob Agents Chemother. 2019 Sep 16;63(12):e01237-19.

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