GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 uM.
CAS：1010411-21-8
分子式：C20H24Cl3N3O
分子量：428.78
纯度：98%
存储：Store at -20°C

Background:

GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 uM.

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 uM[1].

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[1].

参考文献:
[1]. O’Neill PM, et al. Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. J Med Chem. 2009 Mar 12;52(5):1408-15.