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GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.
IC50 value:
Target: NRTI; HIV reverse transcriptase inhibitor
GS-7340 reduces first-pass clearance to be an effective oral prodrug, its permeability and stability were characterized in vitro and detailed pharmacokinetic studies were completed in dogs. GS-7340 showed concentration-dependent permeability through monolayers of caco-2 cells and dose-dependent oral bioavailability in dogs, increasing from 1.7% at 2 mg/kg to 24.7% at 20 mg/kg, suggesting saturable intestinal efflux transport . Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg .. For the detailed information of GS-7340, the solubility of GS-7340 in water, the solubility of GS-7340 in DMSO, the solubility of GS-7340 in PBS buffer, the animal experiment (test) of GS-7340, the cell expriment (test) of GS-7340, the in vivo, in vitro and clinical trial test of GS-7340, the EC50, IC50,and affinity,of GS-7340, Please contact DC Chemicals. |
