MMV009085 is a potent PfHT1 (Plasmodium falciparum hexose transporter)-specific inhibitor and a potential anti-malarial agent . MMV009085 is also a human glucose transporter inhibitor, it has high potency in inhibiting both glucose uptake (IC50: 2.6 μM in glucose uptake assay) and growth of the parasites (EC50: 1.23±0.04 μM against 3D7)[1].
MMV009085 抑制 PfHT-1 转运活性的 IC50 为212±39 μM，抑制 3D7 和 Dd2 生长的 EC50 为1.23±0.04 μM 和 0.720±0.05 μM。此外 MMV009085 对 HEK293T 和 HepG2 细胞的 CC50 值分别为 2.46±0.03 μM 和 1.92±0.85 μM[1]。
MMV009085 在游离寄生虫的葡萄糖摄取实验中显示 IC50 为 2.6 μM; MMV009085 体外抑制恶性疟原虫 3D7 生长的 EC50为 0.987 μM，通过 PfHT 阻断作用抑制疟原虫生长 (EC50=0.795 μM)[1]。
[1]. Xin Jiang, et al. Structural Basis for Blocking Sugar Uptake into the Malaria Parasite Plasmodium falciparum.Cell. 2020 Oct 1;183(1):258-268.e12.