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Beschreibung

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic alpha-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L, 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic alpha-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L, 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).