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UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K ( Pv PI4K) enzyme with an IC 50 of 23 nM In Vitro UCT943 maintains high in vitro selectivity (>200-fold) for the parasite Pv PI4K versus the human PI4Kβ isozyme (IC 50 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 (CC 50 s) of 12, 17, 113, and 13 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 ) 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice with P. berghei and P. falciparum NOD- scid IL-2Rγ (NSG) models Dosage: 10 mg/kg and 3 mg/kg for P. berghei model; 0.01, 0.1, 0.3, 1.1 and 10 mg/kg for P. falciparum NOD- scid IL-2Rγ (NSG) model Administration: Oral administration; daily; 4 days for P. berghei model Oral administration; once per day; 4 days for P. falciparum NOD- scid IL-2Rγ (NSG) model Result: The ED 90 is 1.0 mg/kg in the P. berghei infection model. The ED 90 is 0.25 mg/kg in the P. falciparum -infected NSG mouse model. Form:Solid IC50& Target:Pv PI4K 23 nM (IC 50 ) Plasmodium
中文名称
UCT943
英文名称
UCT943
中文别名
-
英文别名
-
CAS号
1450666-80-4
分子式
C22H20F3N5O
分子量
427.42 g/mol
精确质量
≥98%
PSA
84.100 Ų
Logp
2.400
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MedMol UCT943 98% 5mg

品牌:MedMol
货号:S89611-5mg
级别: -
货期:30天
已售 818 件
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