化合物 CHMFL-PI4K-127 T61971

Product Introduction
Bioactivity


英文名: CHMFL-PI4K-127

描述: CHMFL-PI4K-127 (compound 15g) 是具有口服活性、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂（IC50= 0.9 nM）。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性（EC50= 25.1 nM）。CHMFL-PI4K-127 具有抗疟疾作用。

体外活性: CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase [1]. CHMFL-PI4K-127 exhibits EC 50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum [1].

体内活性: CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model [1]. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 60, 80 mg/kg Administration: Orally, daily for 7 days Result: Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 1, 5, 15 mg/kg Administration: Orally, once Result: Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy.

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

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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