UCT943 是新一代恶性疟原虫 Plasmodium falciparum PI4K 抑制剂。UCT943 抑制 P. vivax PI4K (PvPI4K) 酶，IC₅₀ 为 23 nM。

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC 50 of 23 nM.

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PvPI4K 23 nM (IC50) Plasmodium pan> 

UCT943 maintains high in vitro selectivity (>200-fold) for the parasite Pv PI4K versus the human PI4Kβ isozyme (IC50 of PI4Kβ, 5.4 μM), inhibition of which is linked to immunosuppressive effects.
In vitro cytotoxicity of UCT943 is tested against L6 cells, chinese hamster ovarian (CHO), Vero, and HepG2 cells, with 50% cytotoxic concentrations (CC50s) of 12, 17, 113, and 13 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

UCT943 shows excellent in vivo efficacy in the Plasmodium berghei (10 mg/kg and 3 mg/kg; oral administration; daily; 4 days) and P. falciparum NSG (NOD-scid IL-2Rγ) mouse models (0.01, 0.1, 0.3, 1.1 and 10 mg/kg; oral administration; once per day; 4 days). When dosed at 10 mg/kg per os (p.o.), UCT943 reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice, with >30 mean survival days (MSD). At 3 mg/kg p.o., no complete cure is achieved, and MSD is 10 days, albeit parasitemia is reduced by 99%. The resulting 90% effective dose (ED 90 ) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED 90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model. has not independently confirmed the accuracy of these metho

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Powder -20°C 3 years；4°C 2 years

[1]. Brunschwig C, et al. UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria. Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18.

In Vitro: DMSO : 250 mg/mL (584.90 mM; Need ultrasonic)配制储备液