生物活性 | |||
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描述 | (+)-SJ733 is an anti-malaria agent which can also inhibit Na+-ATPase PfATP4[1]. Acting as an anti-malarial compound, (+)-SJ733 also serves to impede the Na+-ATPase PfATP4 enzyme[1]. The agent attaches itself to a unique receptor on P. falciparum-infected red blood cells, demonstrating a binding affinity equal to its inhibitory effect on growth (kd=50 nM). In comprehensive in vitro analyses and various in vivo dose-regimen studies, (+)-SJ733 revealed no significant safety or tolerability issues across any tested dosages in preclinical models, showcasing a no observed adverse effect level and a maximum tolerated dose exceeding 240 mg/kg from a study over seven days of repeated dosing in rats. Consequently, (+)-SJ733 is projected to possess a safety buffer of at least 43 times[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.67mL 2.13mL 1.07mL |
21.35mL 4.27mL 2.13mL |
参考文献 |
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