E-CFCP

Chemical Structure : E-CFCP

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货号: PC-49649Not For Human Use, Lab Use Only.

E-CFCP is a novel long-acting nucleotide reverse transcriptase inhibitor (NRTI) against HBV, shows potent activity against HBV WTD1 and HBV WTC2 with IC50 of 1.8 and 0.7 nM, respectively.

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生物&药学活性

E-CFCP is a novel long-acting nucleotide reverse transcriptase inhibitor (NRTI) against HBV, shows potent activity against HBV WTD1 and HBV WTC2 with IC50 of 1.8 and 0.7 nM, respectively.
E-CFCP exhibited potent anti-HBV activity in HBV-exposed PXB-cells, blocked the production of intracellular HBV-DNA by IC50qPCR_cell with IC50 of 0.01 nM.
E-CFCP exerted potent activity against ETV-resistant and ADV-resistant HBV variants, HBVETV-RL180M/S202G/M204V (IC50SB_cell=57.2 nM), also potent against HBVADV-RA181T/N236T (IC50SB_cell=6.2 nM).
E-CFCP does not shows significant mtDNA synthesis inhibition in PBMCs and PXB-cells.
Once-daily peroral E-CFCP administration over 2 weeks (0.02∼0.2 mg/kg/day) reduced HBVWTC2-viremia by 2–3 logs in PXB-mice without significant toxicities and the reduction persisted over 1–3 weeks following treatment cessation.

物理化学性质&存储条件

分子量	320.28
分子式	C13H13FN6O3
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	(1S,3S,5S,E)-3-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-2-(fluoromethylene)-5-hydroxy-1-(hydroxymethyl)cyclopentane-1-carbonitrile

参考文献

1. Higashi-Kuwata N, et al. J Hepatol. 2021 May;74(5):1075-1086.

E-CFCP

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E-CFCP

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