货号	规格	价格	上海	北京	珠海	重庆	武汉
S89611-5mg促销	99.30%	￥1700.00 ￥1360.00 S89611-5mg ￥1360.00 现货	6 6	-	-	-	-
S89611-10mg促销	99.30%	￥2970.00 ￥2370.00 S89611-10mg ￥2370.00 现货	8 8	-	-	-	-
S89611-25mg促销	99.30%	￥5100.00 ￥4080.00 S89611-25mg ￥4080.00 现货	5 5	-	-	-	-
S89611-100mg促销	≥98%	￥9870.00 ￥7890.00 S89611-100mg ￥7890.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM

靶点：

PvPI4K:23 nM (IC50);Plasmodium;Parasite; PI4K

体外研究：

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.

体内研究：

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-2Rγnull) 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. Animal Model: Mice with P. berghei and P. falciparum NOD-scid IL-2Rγnull (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-2Rγnull (NSG) model Administration: Oral administration; daily; 4 days for P. berghei modelOral administration; once per day; 4 days for P. falciparum NOD-scid IL-2Rγnull (NSG) model Result: The ED90 is 1.0 mg/kg in the P. berghei infection model. The ED90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.34 ml	11.698 ml	23.396 ml
5 mM	0.468 ml	2.34 ml	4.679 ml
10 mM	0.234 ml	1.17 ml	2.34 ml
50 mM	0.047 ml	0.234 ml	0.468 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

UCT943

(4-(5-amino-6-(4-(trifluoromethyl)phenyl)pyrazin-2-yl)phenyl)(piperazin-1-yl)methanone

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)