化合物INE963 T9741

Product Introduction
Bioactivity


英文名: INE963

描述: INE963 是快速有效的血液阶段抗疟剂，EC50为 3-6 nM。INE963 有单纯性疟疾的研究潜力。

体外活性: INE963 is active against >15 drug-resistant Pf cell lines with EC50’s = 0.5–15 nM. The in vitro log parasite reduction ratio for INE963 is >8.0 at 10 × Pf 3D7 EC50 without a lag phase and a parasite clearance time (PCT99.9) of <24 h. The in vitro selectivity of INE963for Plasmodium vs human cells was exemplified by approximately 1000+ fold shifts against multiple human kinase biochemical assays[1].

体内活性: Following four oral doses at 30 mg/kg of INE963, the frontrunner compounds tested showed significant parasitemia reduction (>99.9%) at day 5 compared to untreated control mice. In addition, the animals did not show any signs of recrudescence of parasite at day 60 post-treatment, indicating complete cure at these doses[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (124.22 mM)


关键字: uncomplicated malaria | inhibit | INE 963 | INE963 | Parasite | antimalarial | INE-963 | Inhibitor

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Parasitic Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途