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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。
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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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 426 | 现货 | |
5 mg | ¥ 987 | 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 x 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | KDU691 is a PI4K inhibitor. |
体内活性 | KDU691 在体内活性方面针对感染了 P. cynomolgi 孢子的恒河猴进行了评估。预防性治疗的猴子没有出现血涂片阳性,而未经治疗的对照组动物显示了正常的寄生虫病发展(初次寄生虫病在感染后第8.9天,第一次复发在一个月内)。因此,感染后不久通过口服20 mg/kg的KDU691进行5天治疗,彻底根除了包括休眠子在内的所有肝阶段寄生虫。 |
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 |
Smiles | CNC(=O)c1ccc(cc1)-c1cnc2cnc(cn12)C(=O)N(C)c1ccc(Cl)cc1 |
密度 | 1.35 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 150 mg/mL (357.26 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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