GSK369796 Dihydrochloride (Synonyms: N-tert-butyl Isoquine) |
カタログ番号GC19183 |
GSK369796 二塩酸塩は、手頃な価格で効果的な抗マラリア薬であり、7.5 μM の IC50 で hERG カリウム イオン チャネルの再分極を阻害します。
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Cas No.: 1010411-21-8
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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