Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KDU691 是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,它是 PI4K 抑制剂,选择性抑制双氢青蒿素预处理的恶性疟原虫。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 462 | 现货 | ||
2 mg | ¥ 668 | 现货 | ||
5 mg | ¥ 996 | 现货 | ||
10 mg | ¥ 1,750 | 现货 | ||
25 mg | ¥ 3,930 | 现货 | ||
50 mg | ¥ 5,630 | 现货 | ||
100 mg | ¥ 7,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,180 | 现货 |
产品描述 | KDU691 is a PI4K inhibitor. |
体内活性 | KDU691 was evaluated for in vivo activity in rhesus macaques infected with P. cynomolgi sporozoites.?The prophylactically treated monkeys failed to become blood smear positive, while untreated control animals showed normal parasitemia development (primary parasitemia at day 8.9 p.i., with the first relapse within a month).?Thus, 5-day oral treatment with 20 mg/kg of KDU691 shortly after infection eradicated all liver-stage parasites, including hypnozoites. |
动物实验 | Sporozoites were harvested from P. cynomolgi-infected mosquitoes, washed with phosphate-buffered saline (PBS), and diluted to 100,000 sporozoites (spz)/ml in PBS. One-milliliter aliquots of sporozoites were prepared and injected into monkeys via intravenous injection. During treatment, monkeys were weighed daily and received the compound via gavage, followed by gastric feeding. Monkeys in the prophylaxis groups were treated 20 min after the i.v. sporozoite injection. The other monkeys were treated when all the monkeys in the experiment (except those in the prophylaxis group) were blood-stage patent (at day 11 p.i.). To kill the blood-stage parasites, all monkeys received a 5-day treatment of 7.5 mg/kg of body weight of chloroquine (CQ), during compound dosing. KDU691 was formulated in 0.5% methylcellulose and 0.5% Tween 80 in water. LMV599 was formulated as a solid dispersion in a solution containing 5.6% (wt/wt) Tween 80 44.4% hydroxypropyl methylcellulose (HPMC) E3 38.9% Soluplus 11.1% vitamin E d-alphatocopheryl polyethylene glycol 1000 succinate. |
分子量 | 419.86 |
分子式 | C22H18ClN5O2 |
CAS No. | 1513879-19-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (357.26 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3817 mL | 11.9087 mL | 23.8175 mL | 59.5437 mL |
5 mM | 0.4763 mL | 2.3817 mL | 4.7635 mL | 11.9087 mL | |
10 mM | 0.2382 mL | 1.1909 mL | 2.3817 mL | 5.9544 mL | |
20 mM | 0.1191 mL | 0.5954 mL | 1.1909 mL | 2.9772 mL | |
50 mM | 0.0476 mL | 0.2382 mL | 0.4763 mL | 1.1909 mL | |
100 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5954 mL |
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。
KDU691 1513879-19-0 Microbiology/Virology PI3K/Akt/mTOR signaling Parasite PI4K PI4 kinases blood Inhibitor liver Phosphatidylinositol 4 kinases ring-stage falciparum plasmodium schizonts gametocytes inhibit KDU 691 KDU-691 stage inhibitor