Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHMFL-PI4K-127 (compound 15g) 是具有口服活性、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂(IC50= 0.9 nM)。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性(EC50= 25.1 nM)。CHMFL-PI4K-127 具有抗疟疾作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM). CHMFL-PI4K-127 shows strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM). CHMFL-PI4K-127 has anti-malaria effect. |
体外活性 | CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase [1]. CHMFL-PI4K-127 exhibits EC 50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum [1]. |
体内活性 | CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model [1]. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 60, 80 mg/kg Administration: Orally, daily for 7 days Result: Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 1, 5, 15 mg/kg Administration: Orally, once Result: Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy. |
分子量 | 402.85 |
分子式 | C18H15ClN4O3S |
CAS No. | 2377604-81-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CHMFL-PI4K-127 2377604-81-2 Inhibitor inhibitor inhibit