UCT943是恶性疟原虫PI4K的抑制剂(IC50 = 23 nM)。
产品描述
UCT943 is an inhibitor of Plasmodium falciparum PI4K (IC50 = 23 nM).
体外活性
UCT943 maintains a high degree of selectivity (>200-fold) for parasite PI4K versus human PI4Kβ isoenzyme (IC50 = 5.4 μM) in vitro, and its inhibition is associated with immunosuppressive effects[1].
体内活性
In vivo, UCT943 shows good efficacy in the Plasmodium vivax (3-10 mg/kg; orally) and P. falciparum NSG mouse models (0.01-10 mg/kg; orally). UCT943 (10 mg/kg; p.o.) reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice (MSD>30)[1].
Cas No.
1450666-80-4
分子式
C22H20F3N5O
分子量
427.42
储存和溶解度
DMSO:250 mg/mL (584.90 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years