Vps34-IN-2

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC 50 s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively Vps34-IN-2 shows antiviral activity against SARS-CoV-2 ( IC 50 of 3.1 μM), HCoV-229E ( IC 50 of 0.7 μM) and HCoV-OC43 . In Vitro Vps34-IN-2 (Compound 31) displays IC 50 s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 exhibits selectivity against mTOR (IC 50 >10 μM) and class I PI3Ks (IC 50 values of 2.7, 4.5, 2.5, and >10 μM on PI3K α, β, δ, γ isoforms, respectively). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo After administration by the intravenous (iv) route, Vps34-IN-2 (Compound 31) concentrations are quantifiable up to 6, 8, and 24 h (last sampling time) depending on animals. After oral administration (po), Vps34-IN-2 is rapidly absorbed with maximal plasma concentrations observed at 0.5 h and a bioavailability of 85%. Slight rebounds of concentrations are observed at 4 and 8 h after oral dosing with no obvious explanation. After iv injection of Vps34-IN-2 at 3 mg/kg, plasma clearance is found moderate (i.e., 2.3 L/h/kg), corresponding to 44% of hepatic blood flow in this species, volume of distribution at steady state is moderate, and terminal elimination half-life is short . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Vps34|2 nM (IC|50|)|SARS-CoV-2|3.1 μM (IC|50|)|HCoV-229E|0.7 μM (IC|50|)

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