| Bioactivity | GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM. |
| Target | IC50: 7.5 μM (hERG potassium ion channel) |
| Invitro | 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[1]. |
| In Vivo | 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]. |
| Name | GSK369796 Dihydrochloride |
| CAS | 1010411-21-8 |
| Formula | C20H24Cl3N3O |
| Molar Mass | 428.78 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |
GSK369796 Dihydrochloride
CAS: 1010411-21-8 F: C20H24Cl3N3O W: 428.78
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolariza
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