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UCT943

CAS No. : 1450666-80-4

MCE 站：UCT943

产品活性：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。

研究领域：PI3K/Akt/mTOR

作用靶点：PI4K

In Vitro: UCT943 maintains high in vitro selectivity (>200-fold) for the parasite PvPI4K 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.

In Vivo: 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^null) 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 (ED₉₀) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED₉₀ is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.

相关产品：Anti-Infection Compound Library  |  Anti-Aging Compound Library  |  Kinase Inhibitor Library  |  Oxygen Sensing Compound Library  |  PI3K/Akt/mTOR Compound Library  |  Glycolysis Compound Library  |  Bioactive Compound Library Plus  |  Cytoskeleton Compound Library  |  PI4KIIIbeta-IN-10  |  PIK-93  |  BF738735  |  PI4KIIIbeta-IN-9  |  PI4KIII beta inhibitor 3  |  KDU691  |  PI-273  |  UCB9608  |  BQR-695  |  T-00127_HEV1  |  KDU731  |  MMV390048

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