Amphihevir

Chemical Structure : Amphihevir

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	448.402
分子式	C21H19F3N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Amphihevir

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物理化学性质&存储条件

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Amphihevir

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