计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
UCT943
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
IC50& Target:Pv PI4K 23 nM (IC 50 ) Plasmodium
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
UCT943
生化机理
UCT943 是新一代恶性疟原虫 PI4K 抑制剂。UCT943 可抑制恶性疟原虫 PI4K（Pv PI4K）酶，IC50 为 23 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CN(CCN1)C(=O)C2=CC=C(C=C2)C3=CN=C(C(=N3)C4=CC=C(C=C4)C(F)(F)F)N
PubChem CID
分子量
427.42
技术文档
高级数据
关联靶点（人）
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(1 活性数据)
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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