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E-CFCP

Chemical Structure : E-CFCP

CAS No.: 2226823-53-4

E-CFCP

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 320.28
Formula C13H13FN6O3
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
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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

References

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

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