GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
IC50&Target
IC50: 7.5 μM (hERG potassium ion channel)
体外研究
In vitro, GSK369796 Dihydrochloride can inhibit the growth of Plasmodium falciparum strains 3D7c, HB3c and K1d, with IC50s of 11.2±2.2, 12.6±5.3 and 13.2±3.2 nM, respectively. Protein binding is higher for GSK369796 Dihydrochloride (compound 4) compare to desethyl amodiaquine in the mouse (93 vs 74%) but similar in human (88 vs 86%). GSK369796 Dihydrochloride can also inhibit hERG potassium ion channel repolarization with an IC50 of 7.5±0.8 μM.
体内研究
In vivo, GSK369796 Dihydrochloride can inhibit the growth of Plasmodium berghei ANKA with ED50 and ED90 of 2.8 and 4.7 mg/kg, respectively.
分子式
C20H24Cl3N3O
分子量
428.78
CAS号
1010411-21-8
运输条件
Room temperature in continental US; may vary elsewhere.