Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM). CHMFL-PI4K-127 shows strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM). CHMFL-PI4K-127 has anti-malaria effect.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM). CHMFL-PI4K-127 shows strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM). CHMFL-PI4K-127 has anti-malaria effect. |
In vitro | CHMFL-PI4K-127 (compound 15g) demonstrates significant selectivity for PfPI4K over human lipid and protein kinases [1]. Furthermore, it exhibits effective half-maximal effective concentration (EC50) values ranging from 23 to 47 nM against various drug-resistant strains of P. falciparum [1]. |
In vivo | CHMFL-PI4K-127 (compound 15g) demonstrated significant antimalarial efficacy in both the blood stage (at a dosage of 80 mg/kg) and liver stage (at 1 mg/kg) of Plasmodium infection in a rodent model when administered orally. Balb/c mice infected with P. yoelii were treated with various dosages for different durations. For the blood stage, doses of 0, 60, and 80 mg/kg were administered daily for 7 days. The highest dose of 80 mg/kg for 7 days produced curative effects, whereas a 60 mg/kg dosage showed suppressive effects during treatment, which relapsed upon cessation. For the liver stage, single doses of 0, 1, 5, and 15 mg/kg were administered, with a 1 mg/kg dose providing full protection and cure, leaving no visible parasites in the liver at multiple time points post-treatment, thus indicating strong causal prophylactic efficacy. |
Molecular Weight | 402.85 |
Formula | C18H15ClN4O3S |
CAS No. | 2377604-81-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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CHMFL-PI4K-127 2377604-81-2 inhibitor inhibit