(+)-SJ733是一种抗疟疾剂,通过抑制 Na+-ATPase PfATP4 来发挥作用,适用于疟疾的治疗和相关研究,展示出其在对抗疟疾病原体中的显著效果。
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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]. |
体内研究 | Administering (+)-SJ733 to mice engineered to lack immune response (NOD-scid IL2Rγnull) and infected with P. falciparum leads to a swift eradication of the parasites, showing an 80% reduction within the first 24 hours and achieving a state where they are undetectable by the 48-hour mark. In a model using the NOD-scid IL2Rγnull mice, when given as four successive daily oral doses, (+)-SJ733 demonstrated remarkable potency and effectiveness against P. falciparum 3D70087/N9 in vivo. It achieved a 90% effective dose (ED90 of 1.9 mg/kg) and drug exposure [area under the curve at ED90 (AUCED90), 1.5 μM⋅h], outperforming artesunate (11.1 mg/kg; AUCED90 unspecified), chloroquine (4.3 mg/kg; AUCED90 3.1 μM⋅h), and pyrimethamine (0.9 mg/kg; AUCED90 5. μM⋅h) in this specific experiment. Following administration of the ED90 dosage, the concentration of (+)-SJ733 in the blood remained higher than the average in vitro EC90 for a duration of 6 to 10 hours post-dose[1]. |
体外研究 | (+)-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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1424799-20-1 |
分子式 | C24H16F4N4O2 |
分子量 | 468.403 |
别名 | SJ000557733 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 50 mg/mL(106.75 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |