ToP-DNJ is a selective endoplasmic reticulum α-glucosidase II ( GluII ) inhibitor with an IC50 value of 9.0 μM. ToP-DNJ selectively inhibits the two catalytic reactions of GluII, and exhibits stronger activity in the first step of converting di-glycosylated glycans to mono-glycosylated glycans. ToP-DNJ exhibits anti- DENV activity. ToP-DNJ can be used in studies related to dengue virus infection [1].
In Vivo, ToP-DNJ (2-10 mg/kg; i.v., p.o.; single dose) preferentially accumulates in the liver of BALB/c mice after both intravenous and oral single-dose administration, with an extended plasma terminal half-life of 8.79 h[1].
In Vitro, ToP-DNJ is a selective inhibitor of isolated endoplasmic reticulum α-glucosidase II, with an IC50 of 9.0 μM, and does not inhibit other tested α- or β-glucosidases at concentrations up to 50 μM[1]. ToP-DNJ inhibits both catalytic reactions of isolated endoplasmic reticulum α-glucosidase II, with higher inhibitory potency against the first reaction (IC50 = 14 μM) than against the second one (IC50 = 56 μM)[1]. ToP-DNJ exhibits anti-dengue virus activity in primary human monocyte-derived macrophages with an IC50 of 12.7 μM[1].
References:
[1]. Kiappes JL, et al. ToP-DNJ, a Selective Inhibitor of Endoplasmic Reticulum α-Glucosidase II Exhibiting Antiflaviviral Activity. ACS Chem Biol. 2018;13(1):60-65.
In Vivo, ToP-DNJ (2-10 mg/kg; i.v., p.o.; single dose) preferentially accumulates in the liver of BALB/c mice after both intravenous and oral single-dose administration, with an extended plasma terminal half-life of 8.79 h[1].
In Vitro, ToP-DNJ is a selective inhibitor of isolated endoplasmic reticulum α-glucosidase II, with an IC50 of 9.0 μM, and does not inhibit other tested α- or β-glucosidases at concentrations up to 50 μM[1]. ToP-DNJ inhibits both catalytic reactions of isolated endoplasmic reticulum α-glucosidase II, with higher inhibitory potency against the first reaction (IC50 = 14 μM) than against the second one (IC50 = 56 μM)[1]. ToP-DNJ exhibits anti-dengue virus activity in primary human monocyte-derived macrophages with an IC50 of 12.7 μM[1].
References:
[1]. Kiappes JL, et al. ToP-DNJ, a Selective Inhibitor of Endoplasmic Reticulum α-Glucosidase II Exhibiting Antiflaviviral Activity. ACS Chem Biol. 2018;13(1):60-65.