产品
编 号：F751735
分子式：C18H15ClN4O3S
分子量：402.85
分子式：C18H15ClN4O3S
分子量：402.85
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CAS No: 2377604-81-2
产品详情
生物活性：
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
体内研究：
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.Animal Model:Balb/c mice were infected by P. yoelii.
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.
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.
体外研究：
CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase.CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum.
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
体内研究：
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.Animal Model:Balb/c mice were infected by P. yoelii.
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.
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.
体外研究：
CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase.CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum.
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