CHMFL-PI4K-127 (compound 15g) 是一种口服有效、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂，IC50为 0.9 nM。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性，其EC50为 25.1 nM。CHMFL-PI4K-127 显示了抗疟疾作用。
| 生物活性 | CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selectivePfPI4K(PlasmodiumfalciparumPI4Kkinase) inhibitor, with anIC50of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7Plasmodiumfalciparum, with anEC50of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy[1]. |
| IC50& Target | PI4K 0.9 ± 0.1 nM (IC50) | PI3Kδ 104 ± 3 nM (IC50) | PI3Kα 191 ± 36 nM (IC50) | PI3Kγ 324 ± 19 nM (IC50) | PI3Kβ 392 ± 27 nM (IC50) | Vps34 681 ± 25 nM (IC50) |
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体外研究
(In Vitro) | CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase[1].
CHMFL-PI4K-127 exhibits EC50values of 23–47 nM against a panel of the drug-resistant strains ofP. falciparum[1].
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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