KDU691  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(150 mg/mL 超声,加热)
产品描述:基本信息 产品编号:K10081 产品名称:KDU691 CAS: 1513879-19-0   储存条件 粉末 -20℃ 四年     分子式: C22H18ClN5O2 溶于液体 -80℃ 两年 分子量 419.86 -20℃ 一个月 化学名:  N-(4-chlorophenyl)-N-methyl-3-[4-(methylcarbamoyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide   Solubility (25°C)   体外 DMSO 84mg/mL (200.06mM) Ethanol 10mg/mL (23.81mM) Water Insoluble 体内 现配现用   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3817mL 11.9087mL 23.8175mL 5mM 0.4763mL 2.3817mL 4.7635mL 10mM 0.2382mL 1.1909mL 2.3817mL 50mM 0.0476mL 0.2382mL 0.4763mL   生物活性 产品描述 一种咪唑吡嗪类药物,对血阶段的裂殖体、配子体和肝期具有较强的抗寄生虫活性,KDU691 是一种 Plasmodium PI4K 抑制剂。 靶点/IC50 PI4K() 体内研究 During the 5 days of dosing, no major weight changes are observed in the animals that receive KDU691 as prophylactic treatment (group 691-proph). From the fourth day of dosing, the animals that are treated with KDU691 show a transient yellow skin color. The KDU691 radical-cure group (group 691-RC) becomes blood-stage positive again at 31.8 days p.i.(range, 31 to 32 days). Clinical chemistry analysis of the group 691-RC monkeys reveals that bilirubin levels accumulate during the 5-day radical-cure treatment with KDU691.     推荐实验方法(仅供参考) 动物实验:   Animal Administration For in vivo PK studies, female CD-1 mice (25 to 30g) are used and randomly assigned to cages. Mice are allowed to acclimate before initiation of the experiments. Feed and water are given ad libitum. KDU691 is formulated at concentrations of 2.5mg/mL and 0.25mg/mL for a dose of 25mg/kg and 2.5mg/kg, respectively. The suspension formulation for p.o. dosing contains 0.5% Methyl cellulose and 0.5% Tween 80 in water. After oral dosing, blood and liver samples from mice are collected at 0.08 to 24h post dosing. Groups of three mice are used for each time point. Blood is centrifuged at 13,000 rpm for 7 min at 4°C, plasma harvested and stored at -20°C until analysis. Liver tissue samples are excised, dipped in PBS, gently blotted with absorbent paper, dried, weighed and stored at -20°C until further analysis.
保存条件:-20℃